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Process for the continuous flow synthesis of ß-amino crotonate (for use in anti-hypertensive drugs)


Project TitleProcess for the continuous flow synthesis of ß-amino crotonate (for use in anti-hypertensive drugs)
Track Codencli-020
Short Description

A process for continuous flow synthesis of >99.98% pure ß- amino crotonates which are intermediates to Calcium Channel Blocker (anti-hypertensive drugs)



ß-amino crotonates are generally produced by a batch synthesis procedure resulting in longer reaction times.


A novel production process for ß-amino crotonate using a continuous mode reactor, with reduced reaction time, yet resulting in higher yield (>93%) and high-purity end-product (>99.98%). The process can be catalytic or catalysis- free : used to produce ß-amino crotonate and its analogues.

• In Asia, an estimated 200 million people suffer from hypertension*
• Calcium channel blockers help to decrease the heart rate, which can further lower the blood pressure, relieve the chest pain and control an irregular beat**- hence their use a hypertensive drugs
• The world market for anti-hypertensive drugs is targeted to exceed $66.2 billion by the year 2015^

*, **,^

• Catalytic as well as a catalyst, free continuous process
• ß amino crotonate yielded is of high purity- process provides a better control on product profile
• Reduced reaction time
• Can be prepared from a variety of amines and beta keto esters

• An intermediate in the synthesis of Ca channel blockers such as amlodipine, nisoladipine, benidipine, nicardipine, etc
• Ca channel blockers are used as intermediates in preparation of anti-hypertensive drugs

• Demonstrated at the lab scale
• On the lookout for potential partners for spin-off and licensing
• Patent application filed: Indian- 1025/DEL/2011

Publication: Joshi, R. A. et al (2012) Continuous flow synthesis of β -amino α, β –unsaturated esters in aqueous medium, Green Process Synth 1, 205-210

Case Manager: Magesh N
Phone: +91-20-25902982

Tagsanti hypertensive, hypertension, beta amino crotonate, calcium channel blockers, continuous flow synthesis, internmediate
Posted DateJul 4, 2012 3:39 AM


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