发明公开
EP1140832A4 PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES
审中-公开
用于生产ARYLPIPERIDINCARBINOL中间体及其衍生物
- 专利标题: PROCESS FOR PREPARING ARYLPIPERIDINE CARBINOL INTERMEDIATES AND DERIVATIVES
- 专利标题(中): 用于生产ARYLPIPERIDINCARBINOL中间体及其衍生物
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申请号: EP99966475申请日: 1999-12-17
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公开(公告)号: EP1140832A4公开(公告)日: 2004-11-03
- 发明人: RONSEN BRUCE , UPADHYAYA SUBHASH P
- 申请人: PENTECH PHARMACEUTICALS INC
- 专利权人: PENTECH PHARMACEUTICALS INC
- 当前专利权人: PENTECH PHARMACEUTICALS INC
- 优先权: US21839398 1998-12-22
- 主分类号: C07C253/30
- IPC分类号: C07C253/30 ; C07C255/41 ; C07D211/78 ; C07D211/22
摘要:
A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II), where X is halogen, C1-C10 alkyl, C1-C10 alkoxy, C1-C10 haloalkyl, hydroxy, or hydrogen; and R2 and R3 each is C1-C4 alkyl and R2 and R3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (-)-trans configuration.
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