发明公开
EP0749410A1 REGIOSPECIFIC PROCESSES TO MAKE CIS-1-AMINO-2-ALKANOL FROM DIOL OR HALOHYDRIN
失效
REGIOSPECIFISCHE工艺的生产顺1-氨基-2-烷醇OFF二醇或卤代醇和
- 专利标题: REGIOSPECIFIC PROCESSES TO MAKE CIS-1-AMINO-2-ALKANOL FROM DIOL OR HALOHYDRIN
- 专利标题(中): REGIOSPECIFISCHE工艺的生产顺1-氨基-2-烷醇OFF二醇或卤代醇和
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申请号: EP95912769.0申请日: 1995-03-07
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公开(公告)号: EP0749410A1公开(公告)日: 1996-12-27
- 发明人: VERHOEVEN, Thomas, R. , ROBERTS, F., Edward , SENANAYAKE, Chris, H. , RYAN, Kenneth. M.
- 申请人: Merck & Co., Inc.
- 申请人地址: 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 专利权人: Merck & Co., Inc.
- 当前专利权人: Merck & Co., Inc.
- 当前专利权人地址: 126, East Lincoln Avenue P.O. Box 2000 Rahway New Jersey 07065-0900 US
- 代理机构: Cole, William Gwyn, et al
- 优先权: US19940212604 19940311
- 国际公布: WO1995024374 19950914
- 主分类号: C07C5
- IPC分类号: C07C5 ; C07C213 ; C07C215
摘要:
A regioselective process for synthesizing any enantiomer of cis-1-amino-2-indanol, or mixture of said enantiomers, from 1,2-indane diol, or 2-halo-1-indanol wherein the process comprises the steps of (a) mixing one equivalent of 1,2-indane diol in a solvent, said solvent selected from an alkyl nitrile or aryl nitrile; (b) adding to the mixture at least about 1,5 equivalents of an acid, said acid selected from a strong protic acid or a Lewis acid or an organic acid, and maintaining thereafter the temperature of the resulting mixture between about -70 °C and about 30 °C for a time period of between about 0.25 hours to about 6.0 hours; and (c) adding excess water to effect hydrolysis, and stirring for a time period of between about 0.5 hour and about 8.0 hours, at a temperature of between about 25 °C and about 80 °C, to give substantially cis-1-amino-2-indanol.
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