| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject compound providing an optically active benzothiepine derivative in high purity and in high yield useful as a raw material compound for a preventive and a therapeutic agent for bone diseases, by reacting a specific benzothiepine derivative with an optically active amine. SOLUTION: A benzothiepine derivative of formula I (R is a lower alkyl) is reacted with an optically active amine. The reaction is preferably carried out by using 0.5-1.0 equivalent of the optically active amine based on the compound of formula I, blending and reacting both the compounds in methanol or tetrahydrofuran and crystallizing or recrystallizing the objective compound. The reaction temperature is 0-30 deg.C and the reaction time is preferably 1-10 hours. A compound of formula II (R<1> is a phenyl which may be replaced; R<2> to R<4> are each H or a lower alkyl; R<5> is H, OH, etc.), especially (1R,2S)- norephedrine is preferable as the optically active amine. The objective compound is deaminated to give an optically active benzothiepine derivative. |
