Gene

Acetylation

Medicinal chemistry

Catalysis

Knoevenagel condensation

Chemistry

Histone deacetylase inhibitor

Histone deacetylase

Pyridine

Benzamide

Biochemistry

Histone

Stereochemistry

Chinese New Drugs Journal

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.

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