公开(公告)号：US06504035B1

公开(公告)日：2003-01-07

申请号：US09959692

申请日：2002-01-28

申请人： Amalija Narandja ,  Nevenka Lopotar ,  Marko Djerek ,  Dra{haeck over (z)}en Pavlović

发明人： Amalija Narandja ,  Nevenka Lopotar ,  Marko Djerek ,  Dra{haeck over (z)}en Pavlović

IPC分类号： C07D32100

CPC分类号： C07H17/08

摘要： The present invention relates to derivatives of 3-deoxy desmycosin of the formula I, wherein, starting from triply protected desmycosin, there are performed an oxidation at C-3 in the first step and then, optionally, a hydrogenation of double bonds and an epoxidation followed by a reductive opening of the oxirane ring. The present invention also relates to derivatives of 3-deoxy-desmycosin of the formula II, wherein in the first step triacetyl desmycosin is hydrogenated and then, via an intermediate mesylate, it is converted to a 2,3-didehydro derivative; or 2,3-didehydro-desmycosin is subjected to epoxidation reactions followed by a reductive opening of the oxirane ring.

摘要翻译： 本发明涉及式I的3-脱氧去糖霉素衍生物，其中，从三重保护的脱沙霉素开始，在第一步中在C-3进行氧化，然后任选地进行双键氢化和环氧化 随后是环氧乙烷环的还原开口。 本发明还涉及式II的3-脱氧 - 去霉霉素的衍生物，其中在第一步中，将三乙酰基脱沙霉素氢化，然后经由甲磺酸中间体转化为2,3-二脱水衍生物; 或2,3-二脱氢脱硫霉素进行环氧化反应，然后进行环氧乙烷环的还原开口。