An Improved Process For Preparation Of Perindopril Intermediate
Patent No. EP2906536 (titled "An Improved Process For Preparation Of Perindopril Intermediate") was filed by Piramal Enterprises on Oct 4, 2013. The application was issued on Mar 14, 2018.
Patent Summary
A process for preparing the key intermediate (2S,3aS,7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)butyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylic acid benzyl ester (Perindopril benzyl ester) used in the synthesis of the ACE inhibitor Perindopril. The process involves reacting the compound of formula III with the compound of formula IV in the presence of 1-hydroxybenzotriazole (HOBT), dicyclohexylcarbodiimide (DCC), and triethylamine in toluene at 5-40°C. The reaction avoids the formation of N-acetyl impurities and completely removes the by-product dicyclohexylurea (DCU), eliminating the need for additional purification steps.
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Date
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EP2906536
- Application Number
- EP13845500A
- Filing Date
- Oct 4, 2013
- Status
- Revoked
- Sep 18, 2020
- Publication Date
- Mar 14, 2018
- External Links
- Slate, Register , Google Patents