| 发明名称 | 埃坡霉素C、其制备方法以及作为细胞抑制剂和植物保护剂的应用 | ||
| 摘要 | 本发明涉及式(I)的埃坡霉素C(R＝氢)及其制备方法，以及其在制备治疗剂和植物保护剂中的应用，所述治疗剂特别是细胞抑制剂。 | ||
| 申请公布号 | CN100344627C | 申请公布日期 | 2007.10.24 |
| 申请号 | CN200510006282.7 | 申请日期 | 1997.11.18 |
| 申请人 | 生物技术研究有限公司(GBF) | 发明人 | 汉斯·赖兴巴赫;格哈德·赫夫勒;克劳斯·格特;海因里希·施泰因梅茨 |
| 分类号 | C07D417/06(2006.01);C12P17/16(2006.01);A01N43/78(2006.01);A61K31/427(2006.01) | 主分类号 | C07D417/06(2006.01) |
| 代理机构 | 永新专利商标代理有限公司 | 代理人 | 张晓威 |
| 主权项 | 1、下式的埃坡霉素C：<img file="C2005100062820002C1.GIF" wi="922" he="469" />埃坡霉素C：R＝H；其经验式为C<sub>26</sub>H<sub>39</sub>NO<sub>5</sub>S，其特征在于具有如表1所示的<sup>1</sup>H-和<sup>13</sup>C-NMR谱：表1：埃坡霉素C在[D<sub>6</sub>]DMSO中于300MHz的<sup>1</sup>H-和<sup>13</sup>C-NMR数据<tables id="table1" num="001"><table width="795"><tgroup cols="4"><colspec colname="c001" colwidth="21%" /><colspec colname="c002" colwidth="29%" /><colspec colname="c003" colwidth="25%" /><colspec colname="c004" colwidth="25%" /><thead><row><entry morerows="1" namest="c001" nameend="c004"> 埃坡霉素C</entry></row></thead><tbody><row><entry morerows="1"> H原子</entry><entry morerows="1"> δ(ppm)</entry><entry morerows="1"> C原子</entry><entry morerows="1"> δ(ppm)</entry></row><row><entry morerows="1"></entry><entry morerows="1"></entry><entry morerows="1"> 1</entry><entry morerows="1"> 170.3</entry></row><row><entry morerows="1"> 2-Ha</entry><entry morerows="1"> 2.38</entry><entry morerows="1"> 2</entry><entry morerows="1"> 38.4</entry></row><row><entry morerows="1"> 2-Hb</entry><entry morerows="1"> 2.50</entry><entry morerows="1"> 3</entry><entry morerows="1"> 71.2</entry></row><row><entry morerows="1"> 3-H</entry><entry morerows="1"> 3.97</entry><entry morerows="1"> 4</entry><entry morerows="1"> 53.1</entry></row><row><entry morerows="1"> 3-OH</entry><entry morerows="1"> 5.12</entry><entry morerows="1"> 5</entry><entry morerows="1"> 217.1</entry></row><row><entry morerows="1"> 6-H</entry><entry morerows="1"> 3.07</entry><entry morerows="1"> 6</entry><entry morerows="1"> 45.4</entry></row><row><entry morerows="1"> 7-H</entry><entry morerows="1"> 3.49</entry><entry morerows="1"> 7</entry><entry morerows="1"> 75.9</entry></row><row><entry morerows="1"> 7-OH</entry><entry morerows="1"> 4.46</entry><entry morerows="1"> 8</entry><entry morerows="1"> 35.4</entry></row><row><entry morerows="1"> 8-H</entry><entry morerows="1"> 1.34</entry><entry morerows="1"> 9</entry><entry morerows="1"> 27.6</entry></row><row><entry morerows="1"> 9-Ha</entry><entry morerows="1"> 1.15</entry><entry morerows="1"> 10</entry><entry morerows="1"> 30.0</entry></row><row><entry morerows="1"> 9-Hb</entry><entry morerows="1"> 1.40</entry><entry morerows="1"> 11</entry><entry morerows="1"> 27.6</entry></row><row><entry morerows="1"> 10-Ha</entry><entry morerows="1"> 1.15<sup>*</sup></entry><entry morerows="1"> 12</entry><entry morerows="1"> 124.6</entry></row><row><entry morerows="1"> 10-Hb</entry><entry morerows="1"> 1.35<sup>*</sup></entry><entry morerows="1"> 13</entry><entry morerows="1"> 133.1</entry></row><row><entry morerows="1"> 11-Ha</entry><entry morerows="1"> 1.90</entry><entry morerows="1"> 14</entry><entry morerows="1"> 31.1</entry></row><row><entry morerows="1"> 11-Hb</entry><entry morerows="1"> 2.18</entry><entry morerows="1"> 15</entry><entry morerows="1"> 76.3</entry></row><row><entry morerows="1"> 12-H</entry><entry morerows="1"> 5.38<sup>**</sup></entry><entry morerows="1"> 16</entry><entry morerows="1"> 137.3</entry></row><row><entry morerows="1"> 13-H</entry><entry morerows="1"> 5.44<sup>**</sup></entry><entry morerows="1"> 17</entry><entry morerows="1"> 119.1</entry></row><row><entry morerows="1"> 14-Ha</entry><entry morerows="1"> 2.35</entry><entry morerows="1"> 18</entry><entry morerows="1"> 152.1</entry></row><row><entry morerows="1"> 14-Hb</entry><entry morerows="1"> 2.70</entry><entry morerows="1"> 19</entry><entry morerows="1"> 117.7</entry></row><row><entry morerows="1"> 15-H</entry><entry morerows="1"> 5.27</entry><entry morerows="1"> 20</entry><entry morerows="1"> 164.2</entry></row><row><entry morerows="1"> 17-H</entry><entry morerows="1"> 6.50</entry><entry morerows="1"> 21</entry><entry morerows="1"> 18.8</entry></row><row><entry morerows="1"> 19-H</entry><entry morerows="1"> 7.35</entry><entry morerows="1"> 22</entry><entry morerows="1"> 20.8</entry></row></tbody></tgroup></table></tables><tables id="table2" num="002"><table width="795"><tgroup cols="4"><colspec colname="c001" colwidth="21%" /><colspec colname="c002" colwidth="29%" /><colspec colname="c003" colwidth="25%" /><colspec colname="c004" colwidth="25%" /><thead><row><entry morerows="1"> 21-H<sub>3</sub></entry><entry morerows="1"> 2.65</entry><entry morerows="1"> 23</entry><entry morerows="1"> 22.6</entry></row></thead><tbody><row><entry morerows="1"> 22-H<sub>3</sub></entry><entry morerows="1"> 0.94</entry><entry morerows="1"> 24</entry><entry morerows="1"> 16.7</entry></row><row><entry morerows="1"> 23-H<sub>3</sub></entry><entry morerows="1"> 1.21</entry><entry morerows="1"> 25</entry><entry morerows="1"> 18.4</entry></row><row><entry morerows="1"> 24-H<sub>3</sub></entry><entry morerows="1"> 1.06</entry><entry morerows="1"> 27</entry><entry morerows="1"> 14.2</entry></row><row><entry morerows="1"> 25-H<sub>3</sub></entry><entry morerows="1"> 0.90</entry><entry morerows="1"></entry><entry morerows="1"></entry></row><row><entry morerows="1"> 26-H<sub>3</sub></entry><entry morerows="1"></entry><entry morerows="1"></entry><entry morerows="1"></entry></row><row><entry morerows="1"> 27-H<sub>3</sub></entry><entry morerows="1"> 2.10</entry><entry morerows="1"></entry><entry morerows="1"></entry></row></tbody></tgroup></table></tables><sup>*</sup>、<sup>**</sup>可互换的归属。 | ||
| 地址 | 联邦德国不伦瑞克 | ||