【药物名称】FR-183998
化学结构式(Chemical Structure):
参考文献No.29359
标题:Benzoylguanidine derivs. as medicaments
作者:Kuno, A.; Mizuno, H.; Yamasaki, K.; Inoue, Y. (Fujisawa Pharmaceutical Co., Ltd.)
来源:JP 1998503770; WO 9604241
合成路线图解说明:

Mitsunobu coupling between boronic acid (I) and 3-bromo-2,5-dichlorothiophene (II) affords the thienyl isophthalate (III). Partial hydrolysis of diester (III) using methanolic KOH gives rise to mono-acid (IV), which is further condensed with N,N-dimethyl ethylenediamine (V) to provide the amide-ester (VI). Displacement of the methyl ester function of (VI) by guanidine (VII) then produces the target acyl guanidine, which is finally converted into the corresponding dihydrochloride salt.

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