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

REGIOSPECIFIC PROCESSES TO MAKE CIS-1-AMINO-2-ALKANOL FROM DIOL OR HALOHYDRIN
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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