| Dorsomorphin的合成 |
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| 引用本文： | 熊正新,陈冬寅,李飞. Dorsomorphin的合成[J]. 合成化学, 2017, 25(6): 531-534. DOI: 10.15952/j.cnki.cjsc.1005-1511.2017.06.16291 |
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| 作者姓名： | 熊正新 陈冬寅 李飞 |
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| 作者单位： | 南京医科大学 药学院，江苏 南京 211166 |
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| 基金项目： | 国家自然科学基金资助项目(21172108):南京医科大学科技发展基金资助项目 |
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| 摘 要： | 以2-氯甲基吡啶盐酸盐为原料，经氰基化、缩合和环合反应制得4-（4-吡啶基）-1H-吡唑-5-胺（5）； 5与2-（4-甲氧基苯基）丙二醛经缩合反应制得化合物6-（4-甲氧基苯基）-3-（4-吡啶基)吡唑并［1,5-a］嘧啶（9）； 9经脱甲基和成醚反应合成了骨形态生成蛋白受体及腺苷酸活化蛋白激酶抑制剂Dorsomorphin,总收率24%，其结构经1H NMR和MS(ESI)确证。
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| 关 键 词： | Dorsomorphin 2-氯甲基吡啶盐酸盐 中间体 药物合成 |
| 收稿时间： | 2016-11-22 |
Synthesis of Dorsomorphin |
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| XIONG Zheng-xin,CHEN Dong-yin,LI Fei. Synthesis of Dorsomorphin[J]. Chinese Journal of Synthetic Chemistry, 2017, 25(6): 531-534. DOI: 10.15952/j.cnki.cjsc.1005-1511.2017.06.16291 |
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| Authors: | XIONG Zheng-xin CHEN Dong-yin LI Fei |
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| Affiliation: | School of Pharmacy, Nanjing Medical University, Nanjing 211166, China |
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| Abstract: | 4-(Pyridin-4-yl)-1 H-pyrazol-5-amine (5) was prepared by cyanation,condensation and cyclization reaction,using 2-(chloromethyl)pyridine hydrochloride as the raw material.6-(4-Methoxy-phenyl)-3-(pyridin-4-yl) pyrazolo [1,5-a] pyrimidine (9) was obtained by condensation of 5 with (4-methoxyphenyl) malondialdehyde.The bone morphogenetic protein receptor and adenosine monophosphate activated protein kinase inhibitor,Dorsomorphin,was successfully synthesized by the sequential demethylation and etherification from 9.The overall yield was 24％.The structure was confirmed by 1H NMR and MS (ESI). |
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| Keywords: | Dorsomorphin 2-(chloromethyl) pyridine hydrochloride intermediate drug synthesis |
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