发明名称 |
Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2<i>H</i>-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto |
摘要 |
The present invention is directed to processes and intermediates useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea (Compound I), crystalline forms and solvate forms thereof; and compositions comprising 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea, crystalline forms and solvate forms thereof prepared by processes as described herein. |
申请公布号 |
US9126946(B2) |
申请公布日期 |
2015.09.08 |
申请号 |
US200913126563 |
申请日期 |
2009.10.27 |
申请人 |
Arena Pharmaceuticals, Inc. |
发明人 |
Carlos Marlon;Dong Weitong;Macias Mark;Sato Suzanne Michiko;Selvey Lee Alani |
分类号 |
A61K31/415;C07C231/16;C07D231/16 |
主分类号 |
A61K31/415 |
代理机构 |
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代理人 |
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主权项 |
1. A process for preparing Form I of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea comprising the step of:
converting an acetonitrile solvate of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea to provide said Form I of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea by removing acetonitrile, wherein said converting comprises reducing solvent content at a temperature sufficient to minimize conversion of said acetonitrile solvate to Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea. |
地址 |
San Diego CA US |