Alkanes Nomenclature, Conformational Analysis, and an Introduction to Synthesis © E.V. Blackburn, 2012 Alkanes • acyclic hydrocarbons • saturated aliphatic hydrocarbons • paraffins • general formula CnH2n+2 © E.V. Blackburn, 2012 Sources of methane • product of anaerobic plant decay • major constituent of natural gas (97%) • “firedamp” of coal mines • “marsh gas” © E.V. Blackburn, 2012 Cycloalkanes Single ring cycloalkanes have the general formula CnH2n thus they have two fewer hydrogen atoms than alkanes. © E.V. Blackburn, 2012 Methane – its structure H sp3 109.5o H H H tetrahedral © E.V. Blackburn, 2012 Methane – its structure H H H H “Fischer Structure” H .. : H :C H .. H “Lewis Structure” © E.V. Blackburn, 2012 Space-filling models Space-filling models depict atoms as spheres and therefore show the volume occupied by atoms and molecules. © E.V. Blackburn, 2012 Ethane - C2H6 1.10Å H sp H H C C H H 1.53Å H 3 A structural formula is a Lewis structure which shows the connectivity of its atoms - the order in which atoms are connected. © E.V. Blackburn, 2012 What is ethane’s structure? Or something in between? © E.V. Blackburn, 2012 Conformations Conformations are structures that are interconvertible by rotation about single bonds. This is the staggered conformation of ethane: This is an example of a sawhorse formula. © E.V. Blackburn, 2012 Newman projections Look along the C-C bond. The nearest carbon masks the rear carbon but all six bonds to the two carbons are visible. The nearest carbon is represented by the point where the three bonds meet. The rear carbon is represented by the circle. staggered eclipsed © E.V. Blackburn, 2012 Space-filling model of ethane staggered eclipsed © E.V. Blackburn, 2012 Potential energy Stability of conformations eclipsed staggered eclipsed 12 kJ/mol 60o 120o 180o rotation © E.V. Blackburn, 2012 Torsional strain Torsional energy is the energy required to rotate the molecule about the C-C bond. The relative instability of the eclipsed conformation is said to be due to torsional strain. © E.V. Blackburn, 2012 Propane - C3H8 H H H H C C C H H H H energy barrier = 14 kJ/mol © E.V. Blackburn, 2012 Butane - C4H10 CH3CH2CH2CH3 (CH3)3CH CH3 H H3C CH3 compound bp mp solubility C2H5OH A -12 -159 1320 B 0C -138 1813 mL/100mL © E.V. Blackburn, 2012 Conformations H 3C H H H H H CH3 H H H CH3 H CH3 H H H CH3 CH3 anti gauche All conformations are free of torsional strain. © E.V. Blackburn, 2012 Stability of conformations H 3C H H H H H CH3 H H H CH3 H CH3 H H H CH3 CH3 anti gauche The methyl groups in the gauche conformations are crowded together and steric repulsion results. These conformations are less stable due to steric strain. © E.V. Blackburn, 2012 Stability of conformations anti gauche © E.V. Blackburn, 2012 Stability of conformations Potential energy H 3C CH3 H3C H3C CH3 H3C H3C H3C CH3 gauche anti 19 kJ 16 kJ 3.8 kJ © E.V. Blackburn, 2012 Nomenclature CH4 methane C2H6 ethane C3H8 propane C4H10 butane Subsequent alkanes are systematically named using a numeric prefix (Greek) (penta-, hexa-, etc.) and the suffix ane. © E.V. Blackburn, 2012 Nomenclature CH4 methane C7H16 heptane C2H6 ethane C8H18 octane C3H8 propane C9H20 nonane C4H10 butane C10H22 decane C5H12 pentane C11H24 undecane C6H14 hexane C12H26 dodecane C13H28 tridecane C14H30 tetradecane C20H42 icosane C100H202 hectane © E.V. Blackburn, 2012 n-Butane CH3CH2CH2CH3 n- - specifies a straight chain hydrocarbon, e.g. nbutane or normal butane (CH3)3CH CH3 H H3C CH3 ? © E.V. Blackburn, 2012 Prefixes...... iso- (CH3)2CHCH3 H3C C CH3 H iso- isobutane © E.V. Blackburn, 2012 Pentane CH3-CH2-CH2-CH2-CH3 n-pentane CH3 CH3-CH-CH 2-CH3 isopentane CH3 CH3-C-CH3 CH3 neopentane CH3 H3C CH3 neo © E.V. Blackburn, 2012 Hexane There are five alkane isomers of formula C6H14 ... © E.V. Blackburn, 2012 n-hexane CH3CH2CH2CH2CH2CH3 © E.V. Blackburn, 2012 isohexane (CH3)2CHCH 2CH2CH3 CH3 H3C C CH2-CH2-CH3 H © E.V. Blackburn, 2012 Neohexane (CH3)3CCH2CH3 CH3 H3C C CH2CH3 CH3 © E.V. Blackburn, 2012 and ........ CH3 CH3-CH-CH-CH 3 CH3 CH3 CH3-CH2-CH-CH 2-CH3 © E.V. Blackburn, 2012 Nomenclature Why not name these more complex alkanes by first identifying and naming the longest carbon chain? – the parent chain. Then consider the groups attached to the parent chain as substituents? © E.V. Blackburn, 2012 Alkyl group substituents An alkyl group is the structure obtained when a hydrogen atom is removed from an alkane. These groups are named by replacing the -ane suffix of the corresponding alkane by -yl, hence “alkyl”. • CH3- methyl (Me-) • CH3CH2- ethyl (Et-) • (CH3)2CH- isopropyl (i-Pr) • CH3CH2CH2- propyl (Pr) © E.V. Blackburn, 2012 Alkyl group substituants • CH3- methyl (Me-) • CH3CH2- ethyl (Et-) • (CH3)2CH- isopropyl (i-Pr) • CH3CH2CH2- propyl (Pr) • CH3CH2CH2CH2- butyl • (CH3)2CHCH2- isobutyl • but …. (CH3)3C- ? • or CH3CHCH2CH3 | © E.V. Blackburn, 2012 alkyl group classification • a “primary” carbon is bonded to one other carbon • a “secondary” carbon is bonded to two carbon atoms • a “tertiary” carbon is bonded to three carbon atoms CH3-CH-CH 2-CH3 sec-butyl CH3 CH3-C-CH3 tert-butyl © E.V. Blackburn, 2012 IUPAC nomenclature • The longest continuous carbon chain forms the basic carbon skeleton. • If there are two of these chains, select the one with the greater number of branch points. • The remaining alkyl groups are considered as substituents. C C C C C C C © E.V. Blackburn, 2012 Nomenclature • The carbon chain is then numbered from the end nearer the first branch point. • The different substituent groups are assigned numbers based on their positions along this chain. • Every substituent must have a number even if they are on the same carbon. • If identical substituents are present use the prefixes di-, tri-, tetra- etc. C C C C C C C 2,3-dimethylpentane not 3,4-dimethylpentane © E.V. Blackburn, 2012 Substituents Substituents are named in alphabetical order. C C C C C C C C C C 4-ethyl-3-methylheptane © E.V. Blackburn, 2012 Hexane CH3-CH2-CH2-CH2-CH2-CH3 CH3 CH3-CH-CH 2-CH2-CH3 CH3 CH3-CH2-C-CH3 CH3 CH3 CH3-CH2-CH-CH 2-CH3 CH3 CH3-CH-CH-CH 3 CH3 © E.V. Blackburn, 2012 Nomenclature of branched alkyl groups Numbering begins at the point where the group is attached to the main chain. © E.V. Blackburn, 2012 Nomenclature of branched alkyl groups © E.V. Blackburn, 2012 Nomenclature of alkyl halides H H3C C CH3 Cl (CH3)3CCl © E.V. Blackburn, 2012 Nomenclature of alcohols Add the suffix ol to the name of longest, linear, carbon chain which includes the carbon bearing the OH and any double or triple C-C bond. CH3CH2OH ethanol H CH3CH2CH2CCH2OH CH2CH3 2-ethyl-1-pentanol The OH group has a higher priority than a multiple CC bond, a halogen, and an alkyl group in determining the carbon chain numbering. © E.V. Blackburn, 2012 Nomenclature of alcohols CH2CH2OH CH3CH2CH2OH 1-propanol 2-phenylethanol CH3H H3C C C CH3 H OH 3-methyl-2-butanol © E.V. Blackburn, 2012 Nomenclature of alcohols OH O H3C C C H OH 2-hydroxypropanoic acid © E.V. Blackburn, 2012 Other nomenclature systems 1. Name the alkyl group followed by the word alcohol: CH3CH2OH ethyl alcohol CH3CHCH 3 OH isopropyl alcohol 2. Name alcohols as derivatives of carbinol, methanol: CH 3OH carbinol OH triphenylcarbinol © E.V. Blackburn, 2012 Vicinal glycols “vicinal” means “adjacent” (vicinus, Latin for adjacent), “glycol” means “diol” Alcohols having two OH groups are called “glycols”: HOCH2CH2OH is ethylene glycol or 1,2-ethanediol © E.V. Blackburn, 2012 Ethers Structure: R-O-R, Ar-O-R, or Ar-O-Ar nomenclature Name the two groups bonded to the oxygen and add the word ether. CH3CH2OCH2CH3 - diethyl ether © E.V. Blackburn, 2012 Nomenclature of ethers O diphenyl ether CH3OCH=CH2 O CH(CH 3)2 CH3CH2CH2CHCH2CH3 | OCH3 methyl vinyl ether isopropyl phenyl ether 3-methoxyhexane © E.V. Blackburn, 2012 Nomenclature of cycloalkanes Cycloalkanes are named by adding the prefix cyclo to the name of the corresponding n-alkane. Br cyclopropane Br 1,3-dibromocyclohexane Br Cl 1-bromo-2-chlorocyclopentane © E.V. Blackburn, 2012 Bicyclic compounds Use the name of the alkane corresponding to the total number of carbons in the rings as the parent: Seven carbons – a bicycloheptane. Now determine the number of carbons in each bridge and place them in the name in order of decreasing length. Bicylo[2.2.1]heptane! © E.V. Blackburn, 2012 Bicyclic compounds bicyclo[2.1.0]pentane bicylco[3.1.1]heptane Number the carbons beginning at one bridgehead, along the longest bridge, then the next longest back to the original bridgehead, then along the shortest bridge. H 3C 7 5 4 3 6 7-methylbicyclo[2.2.1]heptane 1 2 © E.V. Blackburn, 2012 Bicyclic compounds © E.V. Blackburn, 2012 Nomenclature of cyclic ethers Use the prefix oxa- to indicate that an O replaces a CH2 in the ring. oxacyclopropane O O ethylene oxide oxacyclopentane tetrahydrofuran O 1,4-dioxacyclohexane O 1,4-dioxane © E.V. Blackburn, 2012 Nomenclature of alkenes 1. To name alkenes, select the longest carbon chain which includes the carbons of the double bond. Remove the -ane suffix from the name of the alkane which corresponds to this chain. Add the suffix -ene. C C C C C C C C C C a derivative of heptene not octane © E.V. Blackburn, 2012 Nomenclature of alkenes 2. Number this chain so that the first carbon of the double bond has the lowest number possible. 1 C C2 C C C C C C C C 3 4 5 6 7 3-propyl-1-heptene © E.V. Blackburn, 2012 Nomenclature of alkenes 1 3-chlorocyclohexene 2 3 Cl vinyl H H allyl H2C=CHCH 2- H H2C=CHCl H 2C=CHCH 2OH © E.V. Blackburn, 2012 Butene - C4H8 The following are obviously butenes: CH3CH2CH=CH 2 1-butene CH3CH=CHCH 3 2-butene CH3C=CH 2 CH3 methylpropene However there are four alkenes of formula C4H8! compound A B C D bp mp -7C -141C -6C < -195C +1C -106 +4C -139C © E.V. Blackburn, 2012 The butenes - C4H8 compound A B C D bp mp -7C -141C -6C < -195C +1C -106 +4C -139C B, C, and D A H2 Pt, Pd or Ni H2 Pt, Pd or Ni H2/Pt H H CH3CH2CH2CH3 CH3 H3C-C-CH 3 H “A” must be methylpropene! © E.V. Blackburn, 2012 The butenes - C4H8 compound A B C D bp mp -7C -141C -6C < -195C +1C -106 +4C -139C methylpropene i. O3 ii. (CH3)2S B 1. O3 2. (CH3)2S O O H2C=O + CH 3CH2C=O H “B” is 1-butene © E.V. Blackburn, 2012 The butenes - C4H8 compound A B C D bp mp -7C -141C -6C < -195C +1C -106 +4C -139C methylpropene 1-butene 1. O3 C and D 2. (CH3)2S CH3C=O H C and D: CH3CH=CHCH 3 © E.V. Blackburn, 2012 2-butene H3C H C C H CH3 trans H3C CH3 C C H H cis © E.V. Blackburn, 2012 Nomenclature Replace the -ane ending of the parent alkane with -yne. The numbering is analogous to that for alkenes. H C C C2H5 H3C C C CH3 1-butyne 2-butyne H3C C C CH(CH 3)2 4-methyl-2-pentyne © E.V. Blackburn, 2012 Nomenclature “Enynes” are compounds containing both a double and a triple bond. Numbering of the chain starts from the end nearer to the first multiple bond, be it double or triple. CH3 HC CCH2CHCH2CH2CH=CHCH3 4-methyl-7-nonen-1-yne HC CCH2CH2CH=CH 2 1-hexen-5-yne © E.V. Blackburn, 2012 Physical properties of alkanes and cycloalkanes • non-polar • low melting point (-183C for methane) • low boiling point (-161.5C for methane) • colorless • insoluble in water • soluble in non-polar solvents such as petrol, ether, etc. © E.V. Blackburn, 2012 Cyclopropane Ni/H 2 o X 80 Br2/CCl4 H3O+ Y HI CH3CH2CH3 CH2BrCH2CH2Br CH3CH2CH2OH CH3CH2CH2I © E.V. Blackburn, 2012 Cyclobutane H2/Ni o 200 CH3CH2CH2CH3 © E.V. Blackburn, 2012 Relative stabilities of cycloalkanes Baeyer (1885) proposed that rings smaller and larger than cyclopentane were unstable due to angle strain. How does this hypothesis fit the facts? Angle strain in cyclic compounds can be quantitatively evaluated by comparing heats of combustion for each CH2- unit. © E.V. Blackburn, 2012 Heats of combustion/CH2 Cyclane (CH2)n n n-alkane H/n (kJ) 658.6 cyclopropane 3 697.0 cyclobutane 4 686.0 cyclopentane 5 664.0 cyclohexane 6 658.7 cycloheptane 7 662.4 cyclooctane 8 663.8 cyclopentadecane 15 659.0 free of angle strain free of angle strain!!! Why? © E.V. Blackburn, 2012 Cyclanes have puckered, not flat rings: H H H H H H H H cyclobutane H HH H H H H H HH cyclopentane H H H H H H H H H H H H cyclohexane © E.V. Blackburn, 2012 Conformational analysis angle strain Any atom tends to have bond angles that match those of its bonding orbitals: 109.5o for sp3-hybridized carbons. Any deviation from these normal bond angles is accompanied by angle strain. © E.V. Blackburn, 2012 Conformational analysis torsional strain Any pair of sp3 carbons bonded to each other tend to have their bonds staggered. Any deviation from the staggered conformation is accompanied by torsional strain. © E.V. Blackburn, 2012 Conformational analysis - van der Waals strain Non-bonded atoms that just touch one another attract each other. If they are closer, they repel each other. Such crowding is accompanied by van der Waals strain (steric strain). © E.V. Blackburn, 2012 Cyclohexane - the “chair” conformation H H H H H H H H H H H H © E.V. Blackburn, 2012 The “boat” conformation "flag pole" hydrogens 1.83A H H H H H H H H H H H H This conformation is less stable (29.7 kJ/mol) than the chair conformation. It is situated at the top of a PE curve and is therefore a transition state between 2 conformational isomers. © E.V. Blackburn, 2012 Skew-boat conformations H H H H "boat" "skew-boat" The skew-boat conformations are 23.0 kJ/mol less stable than the chair conformation. © E.V. Blackburn, 2012 Conformations of cyclohexane 6.7 kJ E 45 kJ 23 kJ © E.V. Blackburn, 2012 Axial and equatorial hydrogens Ha Ha Ha He He He Ha Ha He He Ha Ha = axial He He= equatorial © E.V. Blackburn, 2012 Axial and equatorial hydrogens Ha Ha He Ha He He He He Ha Ha = axial He Ha Ha He= equatorial © E.V. Blackburn, 2012 Axial and equatorial hydrogens axial equatorial © E.V. Blackburn, 2012 Methylcyclohexane equatorial H H H H H CH3 H H H H H H © E.V. Blackburn, 2012 Methylcyclohexane - axial 1,3 diaxial interaction H CH3 H 3 1 H 3 © E.V. Blackburn, 2012 trans-1,2-dimethylcyclohexane H H H H H CH3 H CH3 H H H H H CH3 H H H H H H H H H CH3 © E.V. Blackburn, 2012 cis-1,2-dimethylcyclohexane H CH3 H H H H H CH3 H H H H H H H H H CH3 H H H H H CH3 © E.V. Blackburn, 2012 cis v trans H H H H H CH3 H CH3 H H H H H CH3 H H H H H CH3 H H H H © E.V. Blackburn, 2012 cis-1,3cis cis © E.V. Blackburn, 2012 trans-1,3- trans © E.V. Blackburn, 2012 trans-1,4- trans ? © E.V. Blackburn, 2012 cis-1,4- cis © E.V. Blackburn, 2012 Nomenclature CH3 Br CH3 OH Br Cl Cl C(CH 3)3 I Br © E.V. Blackburn, 2012 Synthesis of alkanes and cycloalkanes © E.V. Blackburn, 2012 Hydrogenation of alkenes and alkynes H2 CnH2n CnH2n+2 Pt, Pd or Ni alkane alkene H2/Ni C2H5OH 25o, 50 atm (CH3)3CH © E.V. Blackburn, 2012 Hydrogenation of alkenes and alkynes + 2 H2 + H2 Pt Pd © E.V. Blackburn, 2012 Reduction of alkyl halides peroxide RX + Bu3SnH RH + Bu 3SnX Bu = CH 3CH2CH2CH2Bu3SnH = tri-n-butylstannane CH3Cl + Bu3SnD CH3D + Bu3SnCl © E.V. Blackburn, 2012 Alkylation of terminal alkynes An acetylenic hydrogen is weakly acidic: R C C H Na NH 3 (CH3)2CHC C H - R C C Na + + 1/2H2 a sodium acetylide NaNH 2 ether (CH3)2CHC C - Na + + NH 3 © E.V. Blackburn, 2012 Alkylation of terminal alkynes The anion formed will react with a primary halide: R C C- Na + + CH 3X R C CCH 3 + NaX 1. NaNH 2 2. CH3Br H2/Pt © E.V. Blackburn, 2012 Corey – Posner – Whitesides House Synthesis R-X + 2Li 1o, 2o, or 3o 2RLi + CuI diethyl ether R2CuLi + R'X RLi + LiX alkyllithium R2CuLi + LiI lithium dialkylcuprate a Gilman reagent R-R' + RCu +LiX 1o alkyl or 2 o cycloalkyl halide © E.V. Blackburn, 2012 Retrosynthetic analysis target molecule 1st precursor starting compound 2nd precursor Here is a target molecule. Plan a synthesis. CH3CH2CHCH 2CH2CH2CH2CH3 CH3 © E.V. Blackburn, 2012 Retrosynthetic analysis CH3CH2CH CH2CH2CH2CH2CH3 CH3 CH3CH2CH CH3 CuLi BrCH2CH2CH2CH2CH3 2 1. Li 2. CuI CH3CH2CHBr CH3 © E.V. Blackburn, 2012 Retrosynthetic analysis CH3CH2CHBr 1. Li 2. CuI CH3 (CH3CH2CH) 2CuLi CH3 (CH3CH2CH) 2CuLi BrCH2CH2CH2CH2CH3 CH3 CH3CH2CHCH 2CH2CH2CH2CH3 CH3 © E.V. Blackburn, 2012 Corey – Posner – Whitesides House Synthesis Muscalure is the sex pheromone of the common house fly. It is used to attract flies to traps containing insecticide. It can be synthesized by the Corey - House reaction. What lithium dialkylcuprate would you use? H3C(H2C)7 (CH2)7CH2Br H ? H3C(H2C)7 (CH2)12 CH3 H H H Muscalure (CH3(CH2)3CH2)2CuLi © E.V. Blackburn, 2012 Reactions of alkanes with halogens 250-400o C H + X2 Reactivity:- or h C X + HX X2 : F2 > Cl2 > Br2 (> I2) H : 3 o > 2o > 1o > H3C-H © E.V. Blackburn, 2012 Chlorination - a substitution reaction CH4 + Cl2 h or CH3Cl + HCl © E.V. Blackburn, 2012 Polychlorination CH3Cl + Cl2 CH2Cl2 + Cl2 CH2Cl2 + HCl dichloromethane methylene chloride CHCl3 + HCl trichloromethane chloroform CHCl3 + Cl2 CCl4 + HCl tetrachloromethane carbon tetrachloride © E.V. Blackburn, 2012 A Problem? Chlorination leads to the possible formation of four products - a mixture! How can we limit the reaction so that only one product is formed? © E.V. Blackburn, 2012 Bromination Bromination takes place less readily than chlorination but it produces the four analogous brominated products: • bromomethane • dibromomethane -methylene bromide • tribromomethane - bromoform • tetrabromomethane - carbon tetrabromide © E.V. Blackburn, 2012 Iodination and fluorination • iodine does not react • fluorine reacts very readily order of halogen reactivity: F2 > Cl 2 > Br 2 (> I2) © E.V. Blackburn, 2012 A Mechanism • a detailed, step by step, description of the transformation of reagents into products • it must explain all experimental facts • the mechanism should be tested by devising appropriate experiments - mechanistic predictions must be tested in the lab © E.V. Blackburn, 2012 Mechanism of the chlorination of methane The experimental facts 1. No reaction occurs at room temperature in the absence of light. 2. Reaction readily occurs, in the absence of light, at temperatures above 250C. 3. Reaction occurs at room temperature in the presence of light of a wavelength absorbed by chlorine. © E.V. Blackburn, 2012 The experimental facts 4. When the reaction is initiated by light, a large number of chloromethane molecules are produced for each photon of light absorbed by the system. 5. The presence of even a small quantity of oxygen slows down the reaction. © E.V. Blackburn, 2012 The mechanism? 1. Cl Cl 2. Cl 3. H3C h or H CH3 Cl Cl 2Cl CH3 + HCl CH3Cl + Cl 2, 3, 2, 3, 2 etc. © E.V. Blackburn, 2012 Chain Reaction Chain initiation: Cl-Cl 2Cl Chain propagation: Cl + CH 4 CH3 + Cl2 Chain termination: 2Cl 2CH3 Cl + CH 3 CH3 + HCl CH3Cl + Cl Cl2 C2H6 (ethane) CH3Cl © E.V. Blackburn, 2012 Inhibitors CH3 + O2 CH3-O-O a "peroxy" radical A compound which slows down or stops a reaction, even when present in small quantities, is called an inhibitor. © E.V. Blackburn, 2012 Lets test the mecanism If tetraethyllead is heated at 140C...... (C2H5)4Pb Pb + 4C2H5 F. Paneth and W. Hofeditz, Ber., 62, 1335 (1929) © E.V. Blackburn, 2012 An alternative source of chlorine atoms..... (C2H5)4Pb C2H5 + Cl2 140 C Pb + 4C2H5 C2H5Cl + Cl © E.V. Blackburn, 2012 The test (C2H5)4Pb Pb + 4C 2H5 C2H5 + Cl2 C2H5Cl + Cl CH4 + Cl2 140C 0.02% (C2H5)4Pb CH3Cl + HCl © E.V. Blackburn, 2012 Heat of reaction H - CH3 + Cl - Cl Cl - CH3 + H - Cl 438 kJ 351 kJ 243 kJ 681 kJ 432 kJ 783 kJ H = + 438 + 243 - 351 - 432 = -102 kJ © E.V. Blackburn, 2012 Bromination H - CH 3 + Br - Br Br - CH3 + H - Br 438 kJ 293 kJ 193 kJ 631 kJ 366 kJ 659 kJ H = + 438 + 193 - 293 - 366 = -28 kJ © E.V. Blackburn, 2012 Iodination H - CH 3 + I - I 438 kJ 151 kJ I - CH3 + H - I 234 kJ 589 kJ 298 kJ 532 kJ H = + 438 + 151 - 234 - 298 = +57 kJ ENDOTHERMIC!!! © E.V. Blackburn, 2012 Chlorination H = - 102 kJ.......... Cl - Cl 243 kJ Cl + H - CH 3 438 kJ Cl - Cl + CH3 243 kJ H 2Cl 243 kJ Cl - H + CH 3 432 kJ Cl + 6 kJ + Cl - CH 3 351 kJ - 108 kJ © E.V. Blackburn, 2012 How does Cl. react with CH4? In order for chlorination to occur, a Cl. and a CH4 must collide. The H-Cl bond can only form if the two species come in contact. A certain minimum energy must be provided by the collision in order for reaction to occur. Why????? © E.V. Blackburn, 2012 Activation energy Bond breaking and bond formation are not perfectly synchronous processes. Therefore energy liberated during bond formation is not completely available for bond breaking. A collision must therefore provide a certain minimum amount of energy for reaction to occur. This is called the “activation energy”, Ea. © E.V. Blackburn, 2012 Potential energy diagrams Potential energy CH4 + Cl CH3 + HCl Ea = 16.7 kJ H = +6 kJ CH3. + HCl CH4 + Cl Reaction coordinate © E.V. Blackburn, 2012 Potential energy Potential energy diagrams © E.V. Blackburn, 2012 Reaction rates rate = collision x energy factor frequency x probability factor (orientation) © E.V. Blackburn, 2012 Factors affecting collision frequency • concentration • pressure • molecular size • momentum • temperature © E.V. Blackburn, 2012 The probability factor • depends on reactant geometry • depends on the nature of the reaction taking place © E.V. Blackburn, 2012 The energy factor • depends on temperature • depends on activation energy © E.V. Blackburn, 2012 KE distribution among collisions Number of collisions of particular energy E1 E2 > E1 E2 Energy © E.V. Blackburn, 2012 Fraction of collisions with E > Ea = e -Ea/RT © E.V. Blackburn, 2012 Relative rates of reaction rate = collision x energy factor frequency x probability factor (orientation) Cl + CH 3-H HCl + CH 3 H E a (kJ) (kJ) +6 16.7 Br + CH3-H HBr + CH 3 +72 75.3 © E.V. Blackburn, 2012 Relative rates of reaction At 275C, of every 15 million collisions, 375,000 are of sufficient energy to cause reaction when chlorine atoms are involved … and only one is of sufficient energy when bromine atoms are involved. Thus, solely due to Ea differences, the chlorine atom is 375,000 more reactive than the bromine atom. © E.V. Blackburn, 2012 Relative reactivity of halogens X = X2 2X F Cl Br I H = +142 +243 +193 +151 kJ X + CH4 CH3 + HX -134 +6 +72 +140 kJ CH3 + X2 CH3X + X -293 -108 -100 -83 kJ © E.V. Blackburn, 2012 Obed Summit © E.V. Blackburn, 2012 Rate determining step Obed Summit Potential energy Rate determining step Cl + CH4 CH3Cl + Cl Reaction coordinate © E.V. Blackburn, 2012 Transition state Potential energy transition state Ea reagents H products Reaction coordinate © E.V. Blackburn, 2012 Transition state H H C H +X H H H C + HX H H H C H +X H H H C H H H C H +X H H H C H H X H H C + HX H X H H C + HX H © E.V. Blackburn, 2012 Transition state H H C H +X H H H C H H X H H C + HX H H H C H +X H H H C H H X H H C + HX H transition state © E.V. Blackburn, 2012 Transition state + HCl + Cl- ? H + Cl H Cl 1. 2. H Cl - 3. © E.V. Blackburn, 2012 Halogenation CH3CH3 CH3CH3 Cl2 Br2 h CH3CH2Cl chloroethane CH3CH2Br bromoethane © E.V. Blackburn, 2012 Chlorination of propane CH3CH2CH3 Cl2 CH3CH2CH2Cl + CH3CHCH 3 h Cl 1-chloropropane 43% 2-chloropropane 57% © E.V. Blackburn, 2012 Bromination of propane CH3CH2CH3 Br2 CH3CH2CH2Br + CH3CHCH 3 h Br 1-bromopropane 3% 2-bromopropane 97% © E.V. Blackburn, 2012 Halogenation of isobutane CH3 CH3CHCH 3 Cl2 (CH3)2CHCH 2Cl + (CH 3)3CCl h 64% CH3 CH3CHCH 3 Br2 36% (CH3)2CHCH 2Br + (CH 3)3CBr h trace >99% Why this selectivity? © E.V. Blackburn, 2012 Mechanism of the halogenation 1. X2 250-400o 2X initiation or h 2. X + RH HX + R propagation 3. R + X2 RX + X 2, 3, 2, 3, 2, 3....etc. © E.V. Blackburn, 2012 The intermediate alkyl radical The nature of the intermediate free radical determines the product: X CH4 methane CH3CH3 ethane CH3 X2 methyl radical X CH3CH2 ethyl radical CH3X halomethane X2 CH3CH2X haloethane © E.V. Blackburn, 2012 The intermediate alkyl radical CH3CH2CH3 propane X CH3CH2CH2 n-propyl radical CH3CHCH 3 isopropyl radical X2 CH3CH2CH2X 1-halopropane X2 CH3CHXCH 3 2-halopropane © E.V. Blackburn, 2012 Orientation of halogenation abstraction of a primary hydrogen H H H H H C C C C HX H H H H H H H H H C C C C H H H H H H H H C C C C H H H H H abstraction of a secondary hydrogen We have competing reactions and should review factors which influence reaction rates! © E.V. Blackburn, 2012 Reaction rates rate = collision x energy factor frequency x probability factor (orientation) © E.V. Blackburn, 2012 Probability factor The statistical product ratio for the chlorination of propane is 75% 1-chloropropane and 25% 2-chloropropane, a 3:1 mixture. Why? There are three times as many primary hydrogens. However: CH3CH2CH3 Cl2 CH3CH2CH2Cl + CH3CHCH 3 h 43% Cl 57% © E.V. Blackburn, 2012 Relative reactivities Lets look at the relative reactivities per hydrogen atom: tertiary secondary primary Chlorination: 5.0 : 3.8 : 1.0 Bromination: 1600 : 82 : 1 We need to look at activation energies and transition states! © E.V. Blackburn, 2012 Transition state for rate determining step C H+ X C H X C + HX the carbon is developing free radical character So let us look at the stability of free radicals…. © E.V. Blackburn, 2012 Free radical stability H3C-H CH3. + H. H = 438 kJ CH3CH2-H CH3CH2. + H. H = 420 kJ (CH3)2CH-H (CH3)2CH. + H. H = 401 kJ (CH3)3C-H (CH3)3C. + H. H = 390 kJ Order of free radical stability is therefore tertiary > secondary > primary > methyl © E.V. Blackburn, 2012 Free radical stability hyperconjugation Using the concept of resonance:- H H H C C H H H H H C C H H H H H C C H H H H H C C H H A charged system is stabilized when the charge is dispersed or delocalized. Thus the order of free radical stability is tertiary > secondary > primary > methyl. © E.V. Blackburn, 2012 Free radical stability hyperconjugation The electrons are delocalised through overlap of a p orbital which is occupied by one, lone electron, and a orbital of the alkyl group: H H H H H ethyl radical © E.V. Blackburn, 2012 Free radical stability hyperconjugation H H H H H H H H ethyl radical H H H H H H H H H isopropyl radical H H H tert-butyl radical © E.V. Blackburn, 2012 Transition state for rate determining step C H+ X C H X C + HX the carbon is developing free radical character Factors which stabilize free radicals will stabilize the transition state which is developing free radical character. © E.V. Blackburn, 2012 Orientation of halogenation This is determined by the stability of the transition state for the rate determining step. CH3 H3C C CH2 H Br H CH3 H3C C H CH3 E Br Ea1 > Ea2 (CH3)2CHCH 2 Ea1 (CH3)3CH + Br + HBr Ea2 (CH3)3C + HBr (CH3)3CH + Br Reaction coordinate © E.V. Blackburn, 2012 Reactivity and selectivity and the Hammond postulate The postulate states that the transition state resembles the structure of the nearest stable species. Transition states for endothermic steps structurally resemble products whereas transition states for exothermic steps structurally resemble reactants. Thus the later the transition state is attained in the reaction, the more it resembles the products. In other words, the greater the Ea, the more the transition state resembles the products. This will explain the greater selectivity of the bromine atom. © E.V. Blackburn, 2012 Reactivity and selectivity R H + Cl R H Cl R + HCl This reaction has a low activation energy and so the transition state resembles the reactants - it has little radical character. R H + Br R H Br R + HBr The activation energy for the bromination is far higher. The transition state has considerable radical character. The free radical stabilizing factors are far more important in the bromination, hence the greater selectivity. © E.V. Blackburn, 2012 Synthesis of alkanes • Hydrogenation of alkenes and alkynes • Reduction of halides • Corey - Posner, Whitesides – House Synthesis © E.V. Blackburn, 2012 Reactions of alkynes • Alkylation of terminal alkynes • Hydrogenation © E.V. Blackburn, 2012 Reactions of alkanes • Halogenation © E.V. Blackburn, 2012