公开(公告)号：EP0749410A1

公开(公告)日：1996-12-27

申请号：EP95912769.0

申请日：1995-03-07

申请人： Merck & Co., Inc.

发明人： VERHOEVEN, Thomas, R. ,  ROBERTS, F., Edward ,  SENANAYAKE, Chris, H. ,  RYAN, Kenneth. M.

IPC分类号： C07C5 ,  C07C213 ,  C07C215

CPC分类号： C07C213/02 ,  C07C2602/08

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.

摘要翻译： 甲个区域选择性方法是光盘为游离缺失（1R，1S） - 氨基 - （2 S，2 R）链烷醇，特别是（1R，1S） - 氨基 - （2 S，2R） - 茚满醇的合成。