化学
组蛋白脱乙酰基酶
苯甲酰胺
Knoevenagel冷凝
乙酰化
组蛋白脱乙酰酶抑制剂
立体化学
吡啶
组蛋白
生物化学
药物化学
催化作用
基因
出处
期刊:Chinese New Drugs Journal
日期:2004-01-01
被引量:5
摘要
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.
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