(EN) Provided are a method for producing a compound (9) useful as a drug for the treatment of diabetes, and a production intermediate thereof. The method includes steps of (a) synthesizing a diester (3) by reacting a compound (1) and a compound (2), (b) synthesizing an ester (4) by deprotecting the diester (3) (or an ester (4) is synthesized by reacting a compound (5) and the compound (2)), (c) converting the ester (4) into an acid halide, (d) reacting the acid halide with an amidinophenol derivative, and (e) deprotecting the resulting diester derivative under acidic conditions and converting into compound (9). In the formula, R1 represents a halogen atom, R4 represents a lower alkyl group, R5 represents a lower alkyl group, and R12 represents a hydrogen atom or a halogen atom. (ZH) 本发明提供作为糖尿病治疗药物有用的化合物(9)的制造方法及其制造中间体。所述制造方法包括下述工序:(a)通过化合物(1)与化合物(2)的反应,合成二酯(3);(b)通过二酯(3)的脱保护,合成酯(4)(或者通过化合物(5)与化合物(2)的反应合成酯(4));(c)将酯(4)转化为酰卤;(d)使酰卤与脒基苯酚衍生物反应;(e)在酸性条件下对得到的二酯衍生物进行脱保护,转化为化合物(9)。式中,R1表示卤素原子,R4表示低级烷基,R5表示低级烷基,R12表示氢原子或卤素原子。
|