Process for producing trans-4-amino-1-cyclohexanecarboxylic acid derivative
By reacting a base with cis-4-amino-1-cyclohexanecarboxylic acid in an aprotic solvent, the isomerization rate is increased, and the trans isomer is obtained in high yield through a recrystallization step, solving the current problem. The problem of low yield of trans isomer in the technology has been solved, and the efficient production of drug intermediates has been achieved.
CN1821217AInactive Publication Date: 2006-08-23SHIONOGI & CO LTD
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Patent Information
- Application Number
- CN200610059627.X
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2002-03-12
- Filing Date
- 2003-03-07
- Publication Date
- 2006-08-23
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
Technical Problem
It is difficult to effectively produce trans-4-amino-1-cyclohexanecarboxylic acid derivatives with the existing technology, especially due to the low yield of the trans-isomer, which makes it difficult to mass-produce it as a pharmaceutical intermediate.
Method used
By reacting the base with cis-4-amino-1-cyclohexanecarboxylic acid in an aprotic solvent, the isomerization rate is significantly increased and the trans isomer is obtained in high yields via a recrystallization step.
Benefits of technology
The efficient preparation of trans-4-amino-1-cyclohexanecarboxylic acid derivatives is achieved, with an isomerization rate of 90% or higher, and is suitable for the production of pharmaceutical intermediates.
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Abstract
A process for the preparation of Compound (I) comprising reacting Compound (II) with a base in an aprotic solvent, which is represented by the following scheme: wherein R<1> and R<2> are each independently lower alkyl.
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