公开(公告)号：US4017607A

公开(公告)日：1977-04-12

申请号：US597188

申请日：1975-07-18

申请人： Shigeharo Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Takashi Tsuruoka ,  Taro Niida ,  Toyoaki Kawasaki

发明人： Shigeharo Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Takashi Tsuruoka ,  Taro Niida ,  Toyoaki Kawasaki

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08

摘要： As new compounds are provided 9,3",4"-trialkanoyl SF-837 M.sub.1 substances which have therapeutically useful antibacterial activity and do not show any objectionable long-lasting bitter taste upon its oral administration. These 9,3",4"-trialkanoyl SF-837 M.sub.1 substances may be prepared from SF-837 substance, 9,2',3"-tri-acetyl SF-837 M.sub.1 substance, 9,2'-di-acetyl SF-837 substance, 9-propionyl SF-837 substance or 9,2'-dipropionyl SF-837 substance by acylating the latter with an alkanoic acid anhydride at 50.degree.-120.degree. C to produce the corresponding 9,2',3",4"-tetra-alkanoyl SF-837 M.sub.1 substance and occasionally the 9,18,2',3",4"-penta-alkanoyl SF-837 M.sub.1 substance, with involving the shift of the 4"-alkanoyl group to the 3"-hydroxyl group. Partial and selective hydrolysis of the 9,2',3",4"-tetra-alkanoyl SF-837 M.sub.1 substance and/or the 9,18,2',3",4"-penta-alkanoyl SF-837 M.sub.1 substance so produced gives the desired 9,3",4"-tri-alkanoyl SF-837 M.sub.1 substance.

摘要翻译： 当新化合物被提供具有治疗上有用的抗菌活性的9,3“，4” - 三烷酰基SF-837M1物质，并且在其口服给药时不显示任何令人不快的持久苦味。 这些9,3“，4” - 三烷酰基SF-837 M1物质可以由SF-837物质，9,2'，3“ - 三乙酰基SF-837M1物质，9,2'-二 - 乙酰基SF-837物质，9-丙酰基SF-837物质或9,2'-二丙酰基SF-837物质，通过用烷基酸酐在50°-120℃下酰化后者，产生相应的9,2' 3“，4” - 四烷酰基SF-837 M1物质，偶尔有9,18,2'，3“，4” - 五烷酰基SF-837 M1物质，涉及4 “ - 烷酰基与3” - 羟基。 9,2'，3“，4” - 四烷酰基SF-837 M1物质和/或9,18,2'，3“，”4“ - 五烷酰基SF- 837如此生产的M1物质得到所需的9,3“，”4“ - 三烷酰基SF-837 M1物质。