发明名称 |
2-氨基-4,5-二芳基嘧啶类化合物及其制备方法和药物用途 |
摘要 |
2-氨基-4,5-二芳基嘧啶类化合物及其制备方法和药物用途,本发明属于杂环化合物技术领域,涉及到杂环不氢化的含六节环,有两个氮原子作为仅有环杂原子,不与其它环稠合的杂环化合物。在反应釜中加入一种异黄酮,搅拌下加入溶剂和胍,异黄酮与胍摩尔比为1∶1~1∶10,反应液温度为50~100℃,不断滴加碱水溶液,使应体系的pH=8-10,反应5~50小时,得2-取代-4,5-二芳基嘧啶与未反应物的混合物,反应混合物蒸馏至干,加入混合物50~130倍重量1~5%HCl水溶液,加热、溶解、过滤、调至中性、静置、生成沉淀,过滤,得2-氨基-4,5-二芳基嘧啶粗品,该粗品用40~120倍重量的50~80%乙醇溶液重结晶,即得纯品。 |
申请公布号 |
CN101343253A |
申请公布日期 |
2009.01.14 |
申请号 |
CN200810150120.4 |
申请日期 |
2008.06.24 |
申请人 |
陕西师范大学 |
发明人 |
张尊听;高迷想;刘谦光;薛东 |
分类号 |
C07D239/42(2006.01);A61K31/505(2006.01);A61P25/00(2006.01) |
主分类号 |
C07D239/42(2006.01) |
代理机构 |
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代理人 |
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主权项 |
1.下述结构通式1的2-氨基-4,5-二芳基嘧啶化合物1~化合物11,<img file="A2008101501200002C1.GIF" wi="381" he="340" />结构通式1表1化合物1~化合物11的取代基和化学名称<tables num="0001"><table><tgroup cols="9"><colspec colname="c001" colwidth="10%" /><colspec colname="c002" colwidth="8%" /><colspec colname="c003" colwidth="8%" /><colspec colname="c004" colwidth="8%" /><colspec colname="c005" colwidth="8%" /><colspec colname="c006" colwidth="8%" /><colspec colname="c007" colwidth="8%" /><colspec colname="c008" colwidth="8%" /><colspec colname="c009" colwidth="35%" /><thead><row><entry morerows="1"> 化合物</entry><entry morerows="1"> R<sub>1</sub></entry><entry morerows="1"> R<sub>2</sub></entry><entry morerows="1"> R<sub>3</sub></entry><entry morerows="1"> R<sub>4</sub></entry><entry morerows="1"> R<sub>5</sub></entry><entry morerows="1"> R<sub>6</sub></entry><entry morerows="1"> R<sub>7</sub></entry><entry morerows="1"> 化合物的名称</entry></row></thead><tbody><row><entry morerows="1"> 1</entry><entry morerows="1"> i-OPr</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2-羟基-4-异丙氧基苯 基)-5-苯基嘧啶</entry></row><row><entry morerows="1"> 2</entry><entry morerows="1"> i-OPr</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> Br</entry><entry morerows="1"> 2-氨基-4-(2-羟基-3-溴-4-异丙氧基 苯基)-5-苯基嘧啶</entry></row><row><entry morerows="1"> 3</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2,4-二羟基苯基)-5-(4-羟 基苯基)嘧啶</entry></row><row><entry morerows="1"> 4</entry><entry morerows="1"> OMe</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2-羟基-4-甲氧基苯 基)-5-(4-羟基苯基)嘧啶</entry></row><row><entry morerows="1"> 5</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> OMe</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2,4-二羟基苯基)-5-(4-甲 氧基苯基)嘧啶</entry></row><row><entry morerows="1"> 6</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> OH</entry><entry morerows="1"> ON<sub>2</sub></entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2,4-二羟基苯基)-5-(3-硝 基-4-羟基苯基)嘧啶</entry></row><row><entry morerows="1"> 7</entry><entry morerows="1"> OH</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> OH</entry><entry morerows="1"> i-Pr</entry><entry morerows="1"> i-Pr</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2,4-二羟基苯基)-5-(3,5- 二异丙基-4-羟基苯基)嘧啶</entry></row><row><entry morerows="1"> 8</entry><entry morerows="1"> OMe</entry><entry morerows="1"> H</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2,6-二羟基-4-甲氧基苯 基)-5-(4-羟基苯基)嘧啶</entry></row><row><entry morerows="1"> 9</entry><entry morerows="1"> OMe</entry><entry morerows="1"> H</entry><entry morerows="1"> OH</entry><entry morerows="1"> H</entry><entry morerows="1"> OMe</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 氨基-4-(2,6-二羟基-4-甲氧基苯 基)-5-(4-甲氧基苯基)嘧啶</entry></row><row><entry morerows="1"> 10</entry><entry morerows="1"> OMe</entry><entry morerows="1"> OMe</entry><entry morerows="1"> OH</entry><entry morerows="1"> OMe</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2,6-二羟基-3,4-二甲氧基 苯基)-5-(4-甲氧基苯基)嘧啶</entry></row><row><entry morerows="1"> 11</entry><entry morerows="1"> OMe</entry><entry morerows="1"> OMe</entry><entry morerows="1"> OMe</entry><entry morerows="1"> OMe</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> H</entry><entry morerows="1"> 2-氨基-4-(2-羟基-4,5,6-三甲氧基苯 基)-5-(4-甲氧基苯基)嘧啶</entry></row></tbody></tgroup></table></tables>化合物1~化合物11的取代基和化学名称见表1。 |
地址 |
710062陕西省西安市雁塔区长安南路199号 |