公开(公告)号：US4438132A

公开(公告)日：1984-03-20

申请号：US368013

申请日：1982-04-13

申请人： Gaza Galambos ,  Vilmos Simonidesz ,  Istvan Szekely ,  Jozsef Ivanics ,  Krisztina Kekesi ,  Gabor Kovacs ,  Istvan Stadler ,  Peter Kormoczy ,  Karoly Horvath

发明人： Gaza Galambos ,  Vilmos Simonidesz ,  Istvan Szekely ,  Jozsef Ivanics ,  Krisztina Kekesi ,  Gabor Kovacs ,  Istvan Stadler ,  Peter Kormoczy ,  Karoly Horvath

IPC分类号： C07D307/935 ,  A61K31/557 ,  A61P1/04 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  C07C405/00 ,  C07D307/937

CPC分类号： C07D307/937 ,  C07C317/00 ,  Y02P20/55 ,  Y10S514/824 ,  Y10S514/926 ,  Y10S514/927

摘要： The invention relates to a process for the preparation of novel 4-oxo-PGI.sub.2 derivatives of formula I ##STR1## where (a) compounds of formula III ##STR2## are oxidized, then the obtained 5-substituted-4-oxo-PGI.sub.1 derivatives of general formula II ##STR3## are eliminated by the splitting off of the W-H-molecule, or (b) the compounds of formula IV ##STR4## are reacted in a solvent in the presence of a catalyst with compounds of general formula V ##STR5## then the obtained compounds of formula I are transformed if desired by saponification, hydrolysis, salt formation, insertion of a protection group to another compound which belongs to the compounds of formula I, too.The pharmaceutical products of the invention can be used for the treatment of circulatory diseases, they inhibit the aggregation of blood plaques, dilate the bronchi and inhibit the secretion of gastric acid.

摘要翻译： 本发明涉及一种制备式I（I）的新型4-氧代-GII 2衍生物的方法，其中（a）式III的化合物（XIIIX）被氧化，然后得到5-取代的 通过分解WH分子来消除通式II（XIIX）的4-氧代-PGI1衍生物，或（b）式IV化合物（XIVX）在溶剂中在 然后如果需要，通过皂化，水解，形成盐，将保护基团插入另一种属于式（I）化合物的化合物的化合物，转化所得到的式I化合物， 我也。 本发明的药物可用于治疗循环系统疾病，抑制血斑聚集，扩张支气管，抑制胃酸分泌。