DOAJ Open Access 2023

Synthesis and Crystal Structure Analysis of Histone Deacetylase Inhibitor Chidamide

Bo Han Xin-Yan Peng Yan-Qing Gong Jia-Liang Zhong Qing-Wei Zhang

Abstrak

Abstract Chidamide is the first oral subtype-selective histone deacetylase inhibitor approved in China for the treatment of relapsed and refractory peripheral T cell lymphoma. Due to the existence of isomers, many articles or patents have mistaken its structure. Herein we explored the synthesis of the key intermediate (E)-4-((3-(pyridin-3-yl)acrylamido)methyl)benzoic acid (A-3) and chidamide, using the condensing agent HBTU, instead of the unstable N,N'-carbonyldiimidazole. The single crystal of chidamide was determined by X-ray diffraction study. The optimized preparation process was easy to operate, and the purity of the final product can be up to 99.76%. Moreover, the structure of chidamide was established to be (E)-N-(2-amino-4-fluorophenyl)-4-((3-(pyridin-3-yl)acrylamido)methyl)benzamide.

Topik & Kata Kunci

Pharmacy and materia medica

Penulis (5)

Bo Han

Xin-Yan Peng

Yan-Qing Gong

Jia-Liang Zhong

Qing-Wei Zhang

Format Sitasi

APA MLA BibTeX

Han, B., Peng, X., Gong, Y., Zhong, J., Zhang, Q. (2023). Synthesis and Crystal Structure Analysis of Histone Deacetylase Inhibitor Chidamide. https://doi.org/10.1055/s-0043-1768613

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Informasi Jurnal

Tahun Terbit: 2023
Sumber Database: DOAJ
DOI: 10.1055/s-0043-1768613
Akses: Open Access ✓