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Synthesis and Crystal Structure Analysis of Histone Deacetylase Inhibitor Chidamide
- Source :
- Pharmaceutical Fronts, Vol 05, Iss 02, Pp e91-e100 (2023)
- Publication Year :
- 2023
- Publisher :
- Georg Thieme Verlag KG, 2023.
-
Abstract
- 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.
Details
- Language :
- English
- ISSN :
- 26285088 and 26285096
- Volume :
- 05
- Issue :
- 02
- Database :
- Directory of Open Access Journals
- Journal :
- Pharmaceutical Fronts
- Publication Type :
- Academic Journal
- Accession number :
- edsdoj.001b6e7290714639b6777d16d6caf6f0
- Document Type :
- article
- Full Text :
- https://doi.org/10.1055/s-0043-1768613