Cinnamic
acid:
synthesis
of
the
latest
generation
of
angiotensin-converting enzyme inhibitors
ACEI by inhibiting the AngII generation so that the vein dilation, peripheral
resistance decreased, the mean arterial pressure, diastolic and systolic blood pressure
decreased. It applies to the period of high blood pressure, is commonly used
antihypertensive drugs, is one of the best antihypertensive drugs.
Since its inception in the 1970s, angiotensin-converting enzyme inhibitors have
been developed to the second generation. Captopril is the first generation, second
generation non-thiol angiotensin-converting enzyme inhibitors, such as enalapril,
benazepril, in La Puli, lisinopril, perindopril, etc.
Recently, some studies have found that the use of Cinnamic acid as raw materials
to the latest generation of synthetic series of angiotensin-converting enzyme inhibitors
Plymouth drug intermediate 2 - oxo-4 - phenyl butyric acid (OPBA).
The synthesis process is：Cinnamic acid, acrylic acid hydrogenation to be,
obtained after ester of acrylic acid ethyl ester, and then to acrylic acid ethyl ester by
condensation with diethyl oxalate reaction of intermediate 3 - benzyl-2 - oxo-succinic
malonate, and then by dilute sulfuric acid hydrolysis OPBA. Orthogonal experiment
on the synthesis of the key steps OPBA ethyl styrene condensation with diethyl
oxalate - a comprehensive optimization of the hydrolysis reaction, to be suitable
conditions for the synthesis of n (styrene-acrylic acid ethyl ester): n (oxalic acid
diethyl acetate) = 1:3; reaction temperature is 60V; condensation time is 1.5 hours;
hydrolysis time of 15 hours, OPBA yield of 65%.
Cinnamic acid synthesis with the latest generation of angiotensin-converting
enzyme inhibitor drugs, which is characterized protect the heart, kidneys and other
vital organs of the role; Retains potassium, so potassium and diuretics at the same
time the application without an increase in drug or combination of potassium
potassium-sparing diuretics; decline in blood pressure, maintain or increase the vital
organs heart, brain, kidney perfusion.