PREPARATION OF OPTICALLY ACTIVE 3,4-DIHYDROBENZOXAZINE DERIVATIVE

摘要

PURPOSE: Provided is a preparation of optically active 3,4-dihydrobenzoxazine derivative which is an intermediate used in manufacturing antibiotics having a strong antibacterial effect on both gram negative and positive bacteria. CONSTITUTION: Optically active 3,4-dihydrobenzoxazine derivative represented by the formula(I) is manufactured by hydrogenating a compound of the formula(III) with tertiary amine in the presence of metal catalyst to obtain a compound of the formula(II); and reacting the compound of the formula(II) in the presence of a mixture of organic metal catalyst, formic acid and triethylamine, in organic solvent to obtain a compound of the formula(I).