| 发明名称 | Azacitidine process and polymorphs | ||
| 摘要 | The present invention relates to process for the preparation of azacitidine and its crystalline forms. | ||
| 申请公布号 | US9416152(B2) | 申请公布日期 | 2016.08.16 |
| 申请号 | US201414174143 | 申请日期 | 2014.02.06 |
| 申请人 | DR. REDDY'S LABORATORIES LTD.;DR. REDDY'S LABORATORIES, INC. | 发明人 | Cherukupally Praveen;Vujjini Satish Kumar;Varanasi Ganesh;Kandala Sreenadha Charyulu;Areveli Srinivas;Tirumalaraju Satyanarayana Raju |
| 分类号 | C07H19/12;C07H17/02;A61K31/53;C07D405/04;C07H13/12 | 主分类号 | C07H19/12 |
| 代理机构 | Pergament & Cepeda LLP | 代理人 | Pergament & Cepeda LLP ;Cepeda Milagros A.;Pergament Edward D. |
| 主权项 | 1. A process for preparing azacitidine, comprising: a) silylating 5-azacytosine to give a compound of Formula II, wherein R1 is an optionally substituted C1-C5 alkyl group; b) coupling a compound of Formula II with a compound of Formula III: wherein R2 is an optionally substituted acyl or aroyl group, in an ester solvent, in the presence of a non-Lewis Acid compound selected from trifluoromethanesulfonic acid, trichloromethanesulfonic acid, or methanesulfonic acid to provide a compound of Formula V; and c) converting a compound of Formula V to azacitidine by hydrolytic removal of all of the acyl or aroyl groups. | ||
| 地址 | Hyderabad IN | ||