申请人:DAISO CO., LTD.
公开号:EP0841334A1
公开(公告)日:1998-05-13
A novel process for preparing a 1,4 benzodioxane derivative shown by the formula (1) which is a useful intermediate of circulatory drugs and drugs for psychoneurosis, characterized in sulfonating a phenoxypropanediol with a sulfonyl halide, eliminating the protective group, and then cyclizing the sulfonated compound by treating with a base followed by, if necessary, further sulfonation.
In the above formula, R1 is H, RSO2, R is alkyl, phenyl which may be substituted with alkyl, R2, R3, R4 are H, halogen, OH, nitro, cyano, formyl, COOH, alkoxycarbonyloxy, alkyl, alkoxy, haloalkyl, N,N-dialkylamino, alkylcarbonyl, alkoxycarbonyl, phenyl which may be substituted by alkyl, etc.22
一种制备式(1)所示的 1,4-苯并二噁烷衍生物的新工艺,该衍生物是循环系统药物和精神神经药物的有用中间体,其特征在于用磺酰卤磺化苯氧基丙二醇,消除保护基,然后用碱环化磺化化合物,必要时再进行进一步磺化。
在上式中,R1 是 H、RSO2,R 是烷基、可被烷基取代的苯基,R2、R3、R4 是 H、卤素、OH、硝基、氰基、甲酰基、COOH、烷氧基羰氧基、烷基、烷氧基、卤代烷基、N,N-二烷基氨基、烷基羰基、烷氧基羰基、可被烷基取代的苯基等22。