RICHARD J. VARSOLONA
1973 Inverness Drive
Scotch Plains, NJ 07076
varsolona@aol.com
Home: (908) 233-7368
Cell: (908) 403-4498
SUMMARY
PREFORMULATION AND SOLID STATE SCIENTIST with extensive experience in preparing salt forms and polymorphs of NCEs for
early pK profiling. Expert in the area of routine solid-state information such as solubility, thermal characterization (DSC and
TG), XRPD, hygroscopicity and solid-state stability. Also well versed in molecular properties such as Kow and pKa
determinations. Thorougly understand the choice of salt counter-ions to be used for salt screening based on dose and
duration (acute and chronic dosing). Suject Matter Expert in the area of thermodynamics as it relates to polymorphism,
hydrates and solvates and the development of robust crystallization processes. Crystal engineering experience using various
process control variables and wet-milling and sonication techniques. High energy individual devoted to working with crossfunctional teams in areas from discovery to manufacturing. Excellent project management skills with an emphasis on
efficiency, results and documentation.
Professional Experience
PFIZER (FORMERLY WYETH PHARMACEUTICALS), Pearl River, NY
2007-2010
Principal Scientist II
Technical lead for the Chemical Engineering Group in the areas of salt and polymorph screening of new drug candidates.
Developed a strategy for the use of internal resources and external contractors to execute salt and polymorph screening
during the development cycle. Developed and/or improved the crystallization yields, mechanical properties and overall
robustness for three late stage compounds and six Phase I candidates. Performed tech transfers of final crystallization step to
CMOs.
 In one year, oversaw the completion of salt and polymorph screens on 15 new drug candidates and developed
crystallizations for MTD and Phase I delivery to meet early development needs. This required the gathering of solubility
data by HPLC analysis on saturated mother liquors and characterization information on resulting solids using XRPD,
DSC, TG, OM, NMR and/or TG.
 Improved the mechanical properties for a Phase III oncology candidate by altering the final crystallization step and
transferred the technology to Esteve (CMO in Spain).
 Technical lead on polymorph challenge which occurred on a Phase III candidate in the area of Women’s Health at
ZaCH Systems (CMO in Italy). Theorized and proved that this problem could be managed by controlling the level of
impurities present in the final crystallization solvent. As a member of the investigational team, reviewed the quality aspect
of the CMO equipment train during three trips to Italy in 2008. Developed an alternate crystallization to prepare the
desired meta-stable polymorph and maintained routine dialogue with the CMO by supplying updates on a weekly basis.
 Explored new technologies in the area of particle engineering. Demonstrated the use of wet milling in the kilo lab to
achieve the desired particle size on a low melting point compound. Demonstrated the use of in-line sonication techniques
for particles size reduction and to control nucleation.
 Worked closely with the process, analytical and formulation chemists, present results and make decisions on the best
form for development as a member of the solid-state steering committee.
BOEHRINGER INGELHEIM PHARMACEUTICALS, Ridgefield, CT
2001-2007
Senior Principal Scientist
Created the salt and polymorph screening group and staffed the group with one junior level and three senior level scientists.
Enhanced the role of the group from a screening group to an active crystallization development group responsible for the last
step of all new drug candidates being developed at the Ridgefield campus. Solid-state and crystallization expert on project
teams. Improved an amphetamine resolution process for the BI Chemicals plant in Petersburg, VA. Performed tech transfer
for four API crystallizations to the Ingelheim, Germany manufacturing facility. Consultant to R&D facility in Biberach, Germany
and research facility in Laval, Canada. Oversaw multiple API milling steps at Micron Technologies to ensure quality and
particle size requirements.
 Responsible for all aspects of final API relating to crystal form, particle size distribution, morphology and other solidstate properties which may affect the API manufacturing productivity and drug product manufacturing.
 Created and headed the US process development crystallization lab.
 Equipped the lab solid-state characterization equipment such as a TA-DSC1000, TA-TG500, Bruker D8-Discover
XRPD with a Vantec 2000 detector.
 Developed and optimized numerous crystallizations for key process intermediates and all final APIs.
 Developed a crystallization process for an API co-crystal which required tight control of several variables.
 Performed and/or supervised the polymorph/salt screening for all APIs being developed in the US.
 Received the President’s Award for contributions made to a lead LFA candidate.
 Received the Team Spirit Award for work done on the lead diabetes candidate, BI10773.
 Researched several vendors for the purchase of an automated polymorph/salt screening. Purchased the Symyx ®
robotic platform and was responsible for leading the effort across several internal disciplines including purchasing, legal
and building services.
 Championed the external agreement with Avantium to aid in the area of polymorph/salt screening for extensive
polymorph/salt screening studies on late stage compounds to aid in IP protection.
MERCK & CO., INC., Rahway, NJ
1984-2001
Senior Research Chemist (1995-2001)
Responsible for the daily operations of the physical measurements laboratory. Presented solid-state properties information
across interdisciplinary teams. Technical member of the core team which collaborated with Symyx ® Technologies to develop
the well established polymorph and salt screening platform which is currently marketed by Symyx ®. Developed the final API
crystallization step for more than ten APIs in development. Supported the Process Research and Chemical Engineering
groups by supplying thermodynamic stability information for polymorphs/hydrates/solvates and solid-state characterization
information.
 Developed the final crystallization process for the marketed HIV protease inhibitor, Crixivan®.
 Developed and received patents for the novel resolution/racemization process for one of the key chiral intermediates
of Crixivan®.
 Established the storage conditions necessary to prevent the desired ethanol solvate of the API in Crixivan ® from
converting to the undesired hydrate.
 Worked with legal team to help establish a defense against claims of infringement for the crystal forms of the
Fosamax® API from a competitor.
 Supported the development of the marketed product, Aggrestat®.
 Spearheaded Merck’s involvement with Accelrys® in the Polymorph Predictor Consortium. Created and led new
team with members from three departments: Pharmaceutical Sciences, Analytics and Process Development, which
shared costs for Consortium membership.
 Authored the physical properties section in the IND and NDA for over twenty pharmaceutical candidates.
Research Chemist (1990-1995)
Obtained solubility, octanol/water partitioning, pKa, hygroscopicity and solid-state information on relevant polymorphs,
solvates and hydrates. Established phase relationships in the solid-state and solvent processing systems over the intended
operational space for production from pre-development to manufacturing. Supported Process Development and Chemical
Engineering by obtaining physical properties information on samples.
 Developed the final crystallization step for Fosamax® and supported all analytical solid-state activities during
development.
 Established the thermodynamic relationship for several new drug candidates which exhibited polymorphism/hydrate
formation.
 Developed the phase relationships of the two key polymorphs for the API in Proscar® and Propecia®. Supplied key
solubility information for the development of the final novel jet-mixing crystallization process which was used to control the
particle size and avoid a milling step of this known teratogen.
Staff Chemist (1984-1990)
Gathered thermal and physical characterization information of new drug candidates and process intermediates using DSC,
TGA, XRPD, Optical Microscopy, SEM, ight scattering and surface area instrumentation.
 Performed release testing for new drug candidates in development.
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Optimized the kinetic resolution of Ibuprofen L-Lysinate which was being investigated as a fast release version of
Ibuprofen.
Developed a thermal technique for predicting the air oxidation of Zocor® using DSC.
EDUCATION
MS, Analytical/Physical Chemistry, Rutgers University, New Brunswick, NJ
BS, Chemistry, Kean University, Union, NJ
PUBLICATIONS AND PRESENTATIONS
Lorenz, Jon C., Busacca, Carl A., Feng, XuWu, Grinberg, Nelu, Haddad, Nizar, Johnson, Joe, Kapadia, Suresh, Lee, Heewon,
Saha, Anjan, Sarvestani, Max, Spinelli, Earl M., Varsolona, Richard, Wei, Xudong, Zeng, Xinghong and Senanayake, Chris.
Large-Scale Asymmetric Synthesis of a Cathepsin S Inhibitor. The Journal of Organic Chemistry (publication pending)
Gonnella, N.C., Smoliga, John A., Campbell, Scot, Busacca, Carl A., Cerreta, Michael, Varsolona, Richard, and Norwood,
Daniel L. Study and characterization of 5,11-dihydro-11-ethyl-6H-dipyrido(3,2-B:2”,3”-E)(1,4)diazapin-6-one by solid-state
NMR and solution NMR. Journal of Pharmaceutical and Biomedical Analysis Volume 51, 2010 PP1047-1053
Varsolona, Richard J., Polymorphism, Solvates and Hydrates – Understanding The Thermodynamic Relationships of Phases
During The Crystallization/Isolation Of APIs. Organic Process Research and Development, San Diego, CA (2007)
Roschangar, F., Liu, J., Estanove, E., Dulfour, M., Rodriguez, S., Farina, V., Hickey, E., Hossain, A., Jones, P., Lee, H., Lu,
B., Varsolona, R., Schroder, J., Beaulieu, P., Gillard, J., and Senanayake, C. H. Preparartion of 3-substituted-2-pyridin-2ylindoles: regioselectivity of Larock’s inole annulation with 2-alkynylpyridines. Tetrathedron Letters Volume 49 Issue 2.
Busacca, Carl A., Lorenz, Jon C., Grinberg, N., Haddad, N., Hrapchak, M., Latli, B., Lee, H., Sabila, P., Saha, A., Sarvestani,
M., Shen, S., Varsolona, R., Wei, X., and Senanayake, Chris H. A Superior Method for the Reduction of Secondary
Phosphine Oxides. Organic Letters; 2005; 7(19) PP 4277 – 4280
Frutos, Rogelio P., Eriksson, M., Wang, Xiao-Jun, Byrne, D., Varsolona, Richard J., Johnson, Michael D., Nummy, L.,
Krishnamurthy, D., and Senanayake, Chris H. Development of a scalable Process for 1-(3,5-Dichlorophenyl)-5-iodo-3-methyl(4-methylbenzyl)-1H-imidazol[1,2-a]imidazole-2-one: A Key Intermediate for the Synthesis of LFA-1 Inhibitors. Organic
Process Research and Development, Volume 9, No. 2, pp 137 – 140 (2005)
Hansen, Karl B., Chilenski, Jennifer R., Desmond, Richard, Devine, Paul N., Grabowski, Edward J. J., Heid, R., Kubryk, M.,
Mathre, David J. and Varsolona, Richard J. Scalable efficient process for the synthesis of (R)-3,5-bistrifluoromethylphenyl
ethanol via catalytic asymmetric transfer hydrogenation as a DABCO inclusion complex. Tetrahedron : Assymmetry, Volume
14, 3581 -3587 (2003)
Wenslow, Robert M., Baum, Mary W., Ball, Richard G., McCauley, James A. and Varsolona, Richard J. A spectroscopic and
crystallographic study of polymorphism in an aza-steroid. Journal of Pharmaceutical Sciences, Volume 89, No. 10, 1271-1285
(2000)
Crocker, L. S., Varsolona, R. J. and McCauley, J. A.. Two Methods for the Measurement of the Dissociation Pressure of a
Crystalline Hydrate. Journal of Pharmaceutical and Biomedical Analysis 15, 1661 – 1665 (1997)
Chung, J. Y. L., Hughes, D. L., Zhao, D., Song, Z., Mathre, D. J., Ho, G., McNamara, J. M., Douglas, A. W., Reamer, R. A.,
Tsay, F., Varsolona, R. J., McCauley, J. A., Grabowski, E. J. J., Reider, P. J. A Highly Efficient Synthesis of a Fibrogen
Receptor Antagonist L-734,217 via a Novel Chemoselective Sily-Mediated Conjugate Addition of -Lactams to 4Vinylpyridine.The Journal of Organic Chemistry, Volume 61, Number 1, Pages 215 – 222 (1996)
McCauley, J. A., Varsolona, R. J. and Levorse, D. A.. The Effect of Polymorphism and Metastability on the Characterization
and Isolation of Two Pharmaceutical Compounds. Journal of Applied Physics 26, B85-89 (1993)
Prabhu, S. V., Varsolona, R. J., Wehner, T. A., Egan, R. S. and Tway, P. C.. Rapid and Sensitive High-Performance Liquid
Chromatography Method for the Quantitation of Abamectin and Its Delta 8,9 Isomer. Journal of Agriculture and Food
Chemistry 40, Number 4, 622-625 (1992)
Luther, George W., III, Giblin, Anne E., and Varsolona, Richard J. Polarographic analysis of sulfur in marine porewaters.
Limnology and Oceanography, Volume 30, (4), 1985
PATENTS
Besylate salt forms of 1-(5-Tert-Butyl-2-p-Tolyl-2H-Pyrazol-3-YL)-3-(4-(6-Morpholin-4-YL-Methyl)-Pyrid In-3-YL)-Napththalen1-YL-Urea and Polymorphs Thereof – WO/2007/109434
Synthesis of 6,7-Dihydro-5h-Imidazo[1,2-a]imidazole-3-sulfonic acid amides US Patent 20060025447
Crystalline forms of 5,11-Dihydro-11-Ethyl-5-Methyl-8-{2-{(1-Oxido-4-Quinolinyl)Oxy}Ethyl}-6H-Dipyrido [3,2-B:2’,3’-E][1,4]
Diazepin-6-one – WO/2005/097796
Sulfate of an HIV protease inhibitor having an improved oral absorption and bioavailability – WO/1998/054178
Morphological forms of (+)-N-[1,6-Cyano-1,2,3,4-Tetrahydro-2-Naphthalenyl)-3,4-Dihydro-4-Hydroxyspiro[2H-1-Benzopyran-2
-4’-Piperidin]yl] Methanesulfonamide Hydrochloride - WO/1995/023146
New method of preparartion of finasteride – EP 0655458
Dihydroxy open acid salt of simvastatin - EP 1324972
Pyrizanone thrombin inhibitors – US Patent 5866573
Gamma-hydroxy-2-(fluoroallkylaminocarbonyl)-1-piperazinepentanamides and uses thereof – US Patent 6642237
Process for making HIV proteases inhibitors – US Patent 5663341
Polymorphic forms of a growth hormone secretagogue – US Patent 5767124
Process for the production of finasteride – US Patent 5652365
New finasteride process – US patent 5468860
Finasteride Processes – US Patent 5886184
HIV protease inhibitors – US Patent 6071916
Process for making HIV proteases inhibitors – US Patent 5637711
Process for making HIV proteases inhibitors – US Patent 5693803
Thermodynamically stable crystal form of 4"-deoxy-4"-epi-methylamino avermectin B1a/B1b benzoic acid salt and processes
for its preparation – US Patent 6486195