Rapid synthesis of 2-cyanobenzothiazole, isothiocyanate and cyanoformanilide derivatives of dapsone †
作者:Thierry Besson、Jérôme Guillard、Charles W. Rees
DOI:10.1039/a908742g
日期:——
New derivatives of the leprostatic drug dapsone are prepared by way of imino-1,2,3-dithiazoles obtained by condensation of aromatic primary bisamines, including dapsone, with 4,5-dichloro-1,2,3-dithiazolium chloride (Appel salt). Reactions, including microwave irradiation, initiated by nucleophilic attack at different sites of the dithiazole ring transform the bisiminodithiazoles into the symmetrical, and some unsymmetrical, title compounds.
新的麻风药物达普松的衍生物通过将芳香性初级双胺(包括达普松)与4,5-二氯-1,2,3-二噁唑盐(阿佩尔盐)缩合得到的亚氨基-1,2,3-二噁唑来制备。包括微波辐射在内的反应,通过在二噁唑环的不同部位进行亲核攻击,将双亚氨基二噁唑转化为对称的以及一些非对称的目标化合物。