PURPOSE: To obtain the subject new derivative comprising a specific optically active benzothiepin derivative, having bone formation-promoting action and bone absorption-suppressing action, excellent in stability, absorbing property and in bioavailability and useful as a preventing and treating agent, etc., for bone diseases such as osteoporosis.
CONSTITUTION: This new optically active benzothiepin derivative is expressed by formula I (R is a lower alkyl; R1 and R2 are each a lower alkyl or R1 and R2 together form a lower alkylene), has bone formation-promoting action and bone absorption-suppressing action, excellent in stability, absorbing property and bioavailability and useful as a preventing and treating agent, etc., for bone diseases such as osteoporosis. The compound is obtained by reacting an optically active substance of a benzothiepine-2-carboxylic acid derivative expressed by formula II or its derivative reactive in the carboxyl group or its salt with a 4-aminobenzylphosphoic acid diester expressed by formula III in the presence of hydroxybenzotriazole, etc., at 0°C.
TAKETOMI SHIGEHISA
ODA TSUNEO
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