发明名称 Improved Process for the Preparation of Crystalline Form IV of Posaconazole
摘要 The present invention relates to an improved large scale process for the preparation of posaconazole form IV.
申请公布号 US2016168133(A1) 申请公布日期 2016.06.16
申请号 US201414907310 申请日期 2014.07.24
申请人 SANDOZ AG 发明人 Hotter Andreas
分类号 C07D405/14 主分类号 C07D405/14
代理机构 代理人
主权项 1. A process for the preparation of crystalline form IV of posaconazole comprising the steps of: (a) providing a suspension or dispersion of: (i) posaconazole, wherein posaconazole is selected from crystalline form III of posaconazole and(ii) methanol and (b) slurrying the suspension or dispersion at a temperature of 20-30° C.; (c) adding water to the suspension or dispersion, (d) adding posaconazole form IV seed crystals to the suspension or dispersion, (e) slurrying the suspension or dispersion at 40-60° C. until the solvent-mediated solid state transformation to posaconazole form IV is complete, (f) cooling the suspension or dispersion to a temperature of 20-30° C., (g) isolating form IV of posaconazole and (h) drying form IV of posaconazole.
地址 Basel CH