PURPOSE: To provide an optically active 4,1-benzoxazepine derivative expressed by a specific formula, having excellent squalene synthetase inhibiting action and useful as an agent for the prevention and treatment of hypercholesterolemia, an antimycotlc agent, etc.
CONSTITUTION: This benzoxazepine derivative is expressed by formula I (R1 is a lower alkyl; X is H or a metal ion; ring A is a halogen-substituted phenyl; ring B is a lower alkoxy-substituted phenyl), preferably (3R,5S)-7-chloro-5-(2,3- dimethoxyphenyl)-1-neopentyl-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-acetic acid or its Na salt. The derivative is preferably produced by optically resolving a compound of formula II and optionally dissolving the obtained compound and an alkali metal hydroxide in an alcoholic solvent.
TOZAWA RYUICHI
KORI MASAKI
KITANO KAZUAKI
