Invention Grant
US07964749B2 Process for obtaining valine derivatives useful for obtaining a pharmaceutically active compound
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用于获得可用于获得药学活性化合物的缬氨酸衍生物的方法
- Patent Title: Process for obtaining valine derivatives useful for obtaining a pharmaceutically active compound
- Patent Title (中): 用于获得可用于获得药学活性化合物的缬氨酸衍生物的方法
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Application No.: US12090729Application Date: 2006-10-19
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Publication No.: US07964749B2Publication Date: 2011-06-21
- Inventor: Pere Dalmases Barjoan , Joan Huguet Clotet
- Applicant: Pere Dalmases Barjoan , Joan Huguet Clotet
- Applicant Address: ES Castellbisbal
- Assignee: Inke, S.A.
- Current Assignee: Inke, S.A.
- Current Assignee Address: ES Castellbisbal
- Agent Cozen O'Connor
- Priority: ES200502558 20051020
- International Application: PCT/EP2006/067569 WO 20061019
- International Announcement: WO2007/045675 WO 20070426
- Main IPC: C07C233/31
- IPC: C07C233/31 ; C07C305/24
Abstract:
The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an —OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a “one pot” reaction.
Public/Granted literature
- US20100240919A1 Process For Obtaining Valine Derivatives Useful For Obtaining A Pharmaceutically Active Compound Public/Granted day:2010-09-23
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