《中国新药杂志》2004年第06期 作者：尹子卉,吴仲闻,兰玉坤,廖晨钟,山松,李志良,宁志强,鲁先平,李志斌

Synthesis of chidamide,a new histone deacetylase (HDAC) inhibitor

YIN Zi-hui,WU Zhong-wen,LAN Yu-kun,LIAO Chen-zhong, SHAN Song, LI Zhi-liang,NING Zhi-qiang,LU Xian-ping, LI Zhi-bin (Chipscreen Biosciences Ltd . , Shenzhen 518057, China ;Department of Analytical Chemistry , College of Chemistry and Chemical Engineering , Chongqing University, Chongqing 400044, China )  

Objective:To synthesize chidamide {N-(2-amino-5-fluorophenyl)-4-[N-(pyridn-3ylacryloyl) aminomethyl ] benzamide}, a new histone deacetylase (HDAC) inhibitor. Methods: 3-Pyridineacrylic acid was prepared from 3-pyridine carboxaldehyde by Knoevenagel reaction, which was converted to the title compound by 2 steps of acetylation in the presence of N, N'-carbonyl diimida-zole. Results: Chidamide was synthesized in a total yield of 29% . Conclusion: A gentle and easily con-trolled process for synthesis of chidamide is worked out.

目的:合成西达本胺{N-(2-氨基-5-氟苯基)4-[N-(吡啶-3-丙烯酰)氨甲基]苯甲酰胺}.方法:以3-吡啶甲醛为起始原料,通过 Knoevenagel反应,制得吡啶丙烯酸,然后以N,N′-碳酰二咪唑

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