| 发明名称 | 结晶形的美罗培南中间体及美罗培南的制备方法 | ||
| 摘要 | 本发明涉及新结晶形的美罗培南中间体及美罗培南的制备方法。本发明特别涉及式I化合物(4-硝基苄基(4R，5S，6S)-3-({(3S，5S)-5-[(二甲氨基)羰基]-1-[(4-硝基苯氧基)羰基]吡咯烷-3-基}硫代)-6-[(1R)-1-羟乙基]-4-甲基-7-氧-1-氮杂双环[3，2，0]庚-2-烯-2-羧酸酯)的结晶形，以及用于制备式II化合物美罗培南三水合物的改进的方法，式I式II其中，PNB表示对硝基苄基及PNZ表示对硝基苄氧基羰基。 | ||
| 申请公布号 | CN101628914B | 申请公布日期 | 2013.07.17 |
| 申请号 | CN200910150055.X | 申请日期 | 2009.06.30 |
| 申请人 | 吉尼森实验室有限公司 | 发明人 | 阿什文·A·凯姆卡;普拉汶·B·希朱尔;阿莫尔·V·雅瓦哈尔;萨奇·N·谢特;德莫然达·K·帕蒂;尼提·H·卡达姆;哈努曼特·K·杰德哈夫 |
| 分类号 | C07D477/20(2006.01)I;C07D477/06(2006.01)I;A61P31/00(2006.01)I | 主分类号 | C07D477/20(2006.01)I |
| 代理机构 | 北京林达刘知识产权代理事务所(普通合伙) 11277 | 代理人 | 刘新宇;李茂家 |
| 主权项 | 1.一种受保护的美罗培南的结晶形的化合物，其具有以下结构：<img file="FSB00001065384200011.GIF" wi="1155" he="640" />所述化合物包含如下X射线衍射图案：<tables num="0001"><table><tgroup cols="5"><colspec colname="c001" colwidth="19%" /><colspec colname="c002" colwidth="14%" /><colspec colname="c003" colwidth="23%" /><colspec colname="c004" colwidth="14%" /><colspec colname="c005" colwidth="30%" /><tbody><row><entry morerows="1">说明</entry><entry morerows="1">角度</entry><entry morerows="1">d值</entry><entry morerows="1">强度</entry><entry morerows="1">强度％</entry></row><row><entry morerows="1"> </entry><entry morerows="1">2-θ°</entry><entry morerows="1">埃</entry><entry morerows="1">计数</entry><entry morerows="1"> </entry></row><row><entry morerows="1">A＝5.099°</entry><entry morerows="1">5.099</entry><entry morerows="1">17.31756</entry><entry morerows="1">1946</entry><entry morerows="1">100</entry></row><row><entry morerows="1">A＝7.028°</entry><entry morerows="1">7.028</entry><entry morerows="1">12.56692</entry><entry morerows="1">205</entry><entry morerows="1">10.5</entry></row><row><entry morerows="1">A＝10.336°</entry><entry morerows="1">10.336</entry><entry morerows="1">8.55159</entry><entry morerows="1">722</entry><entry morerows="1">37.1</entry></row><row><entry morerows="1">A＝12.515°</entry><entry morerows="1">12.515</entry><entry morerows="1">7.0674</entry><entry morerows="1">143</entry><entry morerows="1">7.4</entry></row><row><entry morerows="1">A＝12.824°</entry><entry morerows="1">12.824</entry><entry morerows="1">6.89778</entry><entry morerows="1">196</entry><entry morerows="1">10.1</entry></row><row><entry morerows="1">A＝13.120°</entry><entry morerows="1">13.12</entry><entry morerows="1">6.74238</entry><entry morerows="1">233</entry><entry morerows="1">12</entry></row><row><entry morerows="1">A＝13.460°</entry><entry morerows="1">13.46</entry><entry morerows="1">6.57325</entry><entry morerows="1">266</entry><entry morerows="1">13.7</entry></row><row><entry morerows="1">A＝13.935°</entry><entry morerows="1">13.935</entry><entry morerows="1">6.35002</entry><entry morerows="1">287</entry><entry morerows="1">14.7</entry></row><row><entry morerows="1">A＝14.148°</entry><entry morerows="1">14.148</entry><entry morerows="1">6.25482</entry><entry morerows="1">313</entry><entry morerows="1">16.1</entry></row><row><entry morerows="1">A＝15.472°</entry><entry morerows="1">15.472</entry><entry morerows="1">5.72235</entry><entry morerows="1">832</entry><entry morerows="1">42.7</entry></row><row><entry morerows="1">A＝15.751°</entry><entry morerows="1">15.751</entry><entry morerows="1">5.62166</entry><entry morerows="1">463</entry><entry morerows="1">23.8</entry></row></tbody></tgroup></table></tables><tables num="0002"><table><tgroup cols="5"><colspec colname="c001" colwidth="21%" /><colspec colname="c002" colwidth="15%" /><colspec colname="c003" colwidth="25%" /><colspec colname="c004" colwidth="15%" /><colspec colname="c005" colwidth="24%" /><tbody><row><entry morerows="1">A＝16.987°</entry><entry morerows="1">16.987</entry><entry morerows="1">5.21529</entry><entry morerows="1">1407</entry><entry morerows="1">72.3</entry></row><row><entry morerows="1">A＝17.561°</entry><entry morerows="1">17.561</entry><entry morerows="1">5.0462</entry><entry morerows="1">615</entry><entry morerows="1">31.6</entry></row><row><entry morerows="1">A＝18.335°</entry><entry morerows="1">18.335</entry><entry morerows="1">4.83496</entry><entry morerows="1">482</entry><entry morerows="1">24.8</entry></row><row><entry morerows="1">A＝19.085°</entry><entry morerows="1">19.085</entry><entry morerows="1">4.64653</entry><entry morerows="1">230</entry><entry morerows="1">11.8</entry></row><row><entry morerows="1">A＝19.719°</entry><entry morerows="1">19.719</entry><entry morerows="1">4.49848</entry><entry morerows="1">519</entry><entry morerows="1">26.7</entry></row><row><entry morerows="1">A＝20.101°</entry><entry morerows="1">20.101</entry><entry morerows="1">4.41393</entry><entry morerows="1">445</entry><entry morerows="1">22.8</entry></row><row><entry morerows="1">A＝20.769°</entry><entry morerows="1">20.769</entry><entry morerows="1">4.27349</entry><entry morerows="1">777</entry><entry morerows="1">39.9</entry></row><row><entry morerows="1">A＝22.112°</entry><entry morerows="1">22.112</entry><entry morerows="1">4.0168</entry><entry morerows="1">226</entry><entry morerows="1">11.6</entry></row><row><entry morerows="1">A＝22.541°</entry><entry morerows="1">22.541</entry><entry morerows="1">3.94135</entry><entry morerows="1">595</entry><entry morerows="1">30.6</entry></row><row><entry morerows="1">A＝23.300°</entry><entry morerows="1">23.3</entry><entry morerows="1">3.81463</entry><entry morerows="1">622</entry><entry morerows="1">32</entry></row><row><entry morerows="1">A＝24.031°</entry><entry morerows="1">24.031</entry><entry morerows="1">3.70026</entry><entry morerows="1">458</entry><entry morerows="1">23.5</entry></row><row><entry morerows="1">A＝24.885°</entry><entry morerows="1">24.885</entry><entry morerows="1">3.5751</entry><entry morerows="1">188</entry><entry morerows="1">9.7</entry></row><row><entry morerows="1">A＝25.345°</entry><entry morerows="1">25.345</entry><entry morerows="1">3.51129</entry><entry morerows="1">282</entry><entry morerows="1">14.5</entry></row><row><entry morerows="1">A＝26.421°</entry><entry morerows="1">26.421</entry><entry morerows="1">3.37066</entry><entry morerows="1">363</entry><entry morerows="1">18.7</entry></row><row><entry morerows="1">A＝27.525°</entry><entry morerows="1">27.525</entry><entry morerows="1">3.23795</entry><entry morerows="1">236</entry><entry morerows="1">12.1</entry></row><row><entry morerows="1">A＝28.925°</entry><entry morerows="1">28.925</entry><entry morerows="1">3.08437</entry><entry morerows="1">217</entry><entry morerows="1">11.1</entry></row><row><entry morerows="1">A＝31.233°</entry><entry morerows="1">31.233</entry><entry morerows="1">2.8615</entry><entry morerows="1">130</entry><entry morerows="1">6.7</entry></row></tbody></tgroup></table></tables>。 | ||
| 地址 | 印度新孟买 | ||