Invention Grant
US5952498A Process for the preparation of enantiomerically pure cycloalkano-indol
-and azaindol -and pyrimido �1,2a! indolcarboxcyclic acids and their
activated derivatives
失效
制备对映异构纯的环烷基 - 吲哚 - 和氮杂吲哚和嘧啶并[1,2a]吲哚羧酸及其活化衍生物的方法
- Patent Title: Process for the preparation of enantiomerically pure cycloalkano-indol -and azaindol -and pyrimido �1,2a! indolcarboxcyclic acids and their activated derivatives
- Patent Title (中): 制备对映异构纯的环烷基 - 吲哚 - 和氮杂吲哚和嘧啶并[1,2a]吲哚羧酸及其活化衍生物的方法
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Application No.: US829566Application Date: 1997-03-31
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Publication No.: US5952498APublication Date: 1999-09-14
- Inventor: Jan-Bernd Lenfers , Peter Fey , Paul Naab , Kai Van Laak
- Applicant: Jan-Bernd Lenfers , Peter Fey , Paul Naab , Kai Van Laak
- Applicant Address: DEX Leverkusen
- Assignee: Bayer Aktiengesellschaft
- Current Assignee: Bayer Aktiengesellschaft
- Current Assignee Address: DEX Leverkusen
- Priority: DEX19613549 19960404
- Main IPC: C07C69/612
- IPC: C07C69/612 ; C07C69/616 ; C07C69/65 ; C07D471/04 ; C07D487/04
Abstract:
The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido�1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido�1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.
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