以2-甲基-6-苯基-3-(2,4-二氯苯基)-5,7-二羟基吡唑并[1,5-a]嘧啶为原料,经三氯氧磷氯代得到2-甲基-6-苯基-3-(2,4-二氯苯基)-5,7-二氯吡唑并[1,5-a]嘧啶,氯代物再与胺类化合物经取代反应氨化得到12个未见文献报道的7-取代-3,6-二芳基取代吡唑并[1,5-a]嘧啶类衍生物.目标化合物结构经红外光谱、核磁共振氢谱、元素分析及单晶X射线衍射法表征.
参考文献
| [1] | Portilla J,Quiroga J,Nogueras M,et al.Regioselective Synthesis of Fused Pyrazolo[1,5-a]pyrimidines by Reaction of 5-Amino-1H-pyrazoles and β-Dicarbonyl Compounds Containing Five-membered Rings[J].Tetrahedron,2012,68 (4):988-994 and references therein. |
| [2] | Fraley M E,Hoffman W F,Rubino R S,et al.Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5-a]pyrimidines:A New Class of KDR Kinase Inhibitors[J].Bioorg Med Chem Lett,2002,12:2767-2770. |
| [3] | Fraley M E,Rubino R S,Hoffman W F,et al.Optimization of a Pyrazolo[1,5-a]pyrimidine Class of KDR Kinase Inhibitors:Improvements in Physical Properties Enhance Cellular Activity and Pharmacokinetics[J].Bioorg Med Chem Lett,2002,12:3 5 3 7-3 541. |
| [4] | Frey R R,Curtin M L,Albert D H,et al.7-Aminopyrazolo[1,5-a]pyrimidines as Potent Multitargeted Receptor Tyrosine Kinase Inhibitors[J].J Med Chem,2008,51(13):3777-3787. |
| [5] | Machrouhi F,Ouhamou N,Laderoute K,et al.The Rational Design of a Novel Potent Analogue of the 5'-AMP-Activated Protein Kinase Inhibitor Compound C with Improved Selectivity and Cellular Activity[J].Bioorg Med Chem Lett,2010,20:6394-6399. |
| [6] | LIU Ju,WANG Yang,JIANG Mingjun,et al.Synthesis of 6-Arylsubstitued Pyrazolo[1,5-a]pyrimidine[J].Liaoning Univ (Nat Sci),2011,38(4):319-322(in Chinese).刘举,王洋,姜明俊,等.6-芳基取代吡唑并[1,5-a]嘧啶的合成[J].辽宁大学学报(自然科学版),2011,38(4):319-322. |
| [7] | WANG Zheng.Studies on Synthesis and Anti-tumor Activity of Adamantane Analogs[D].Shenyang:Liaoning University,2012(in Chinese).王正.金刚烷类化合物的合成及其抗肿瘤活性研究[D].沈阳:辽宁大学,2010. |
上一张
下一张
上一张
下一张
计量
- 下载量()
- 访问量()
文章评分
- 您的评分：
-
10%
-
20%
-
30%
-
40%
-
50%