公开(公告)号：US4045479A

公开(公告)日：1977-08-30

申请号：US598995

申请日：1975-07-25

申请人： Friedrich Asinger ,  Heribert Offermanns ,  Karl-Heinz Gulzek

发明人： Friedrich Asinger ,  Heribert Offermanns ,  Karl-Heinz Gulzek

IPC分类号： C07D277/06 ,  C07D277/10 ,  C07C99/00

CPC分类号： C07D277/06 ,  C07D277/10

摘要： Penicillamine or a homolog thereof is made by reacting an aldehyde branched at the .alpha.-carbon atom, sulfur and ammonia to form a thiazoline- .DELTA..sup.3 ; converting the latter compound by reaction with anhydrous hydrogen cyanide into the corresponding thiazolidine-4-carbonitrile; hydrolyzing the nitrile with an aqueous concentrated hydrochloric acid containing at least 30% by weight of hydrogen chloride at a temperature between 40.degree. and 70.degree. C to form the hydrochloric salt of the thiazolidine-4-acid amide and then, at a higher temperature continuing the hydrolysis to form the salt of the thiazolidine-4-carboxylic acid together with the ammonium salt. The ammonium salt is then separated from the mixture and the carboxylic acid hydrochloride is hydrolytically decomposed whereby the penicillamine is obtained.

摘要翻译： 青霉胺或其同系物通过使在α-碳原子上分支的醛，硫和氨反应形成噻唑啉-TATA 3而制备; 通过与无水氰化氢反应将后一种化合物转化成相应的噻唑烷-4-腈; 在40℃〜70℃的温度下，用含有至少30重量％氯化氢的浓盐酸水解腈，形成噻唑烷-4-酸酰胺的盐酸盐，然后在更高的温度下继续 水解形成噻唑烷-4-羧酸的盐与铵盐一起。 然后将铵盐与混合物分离，并将羧酸盐酸盐水解分解，从而得到青霉胺。