PROCESS AND INTERMEDIATES FOR SORBINIL

摘要

Chiral sorbinil intermediates of the formula (wherein R is hydrogen or benzyloxycarbonyl and Y is hydroxy or amino) are useful as intermediates for the preparation of sorbinil. The compound of the formula in which R is benzyloxycarbonyl and Y is amino can be treated with a strong base to convert to sorbinil of the formula: The chiral intermediates may be produced by a process which involves combining racemic 6-fluoro-4-(benzyloxycarbonylamino)-chroman-4-carboxylic acid with 1-(-)-alpha-methylbenzylamine and then resolving the resulting salt.