4.6 Article

Development of an Efficient New Route to PPARδ Agonist Fonadelpar: Formation of the C-C Bond by Claisen Condensation

期刊

ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 26, 期 10, 页码 2900-2907

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.2c00235

关键词

PPAR delta agonist; fonadelpar; ethylene; Claisen-Schmidt condensation

资金

  1. LiaoNing Revitalization Talents Program [XLYC1902089]
  2. General Scientific Research Projects of Department of Education in Liaoning Province [LJKQZ2021032, LJKZ0930]

向作者/读者索取更多资源

This article presents an efficient new synthesis method for a peroxisome proliferator-activated receptor delta agonist fonadelpar. The method utilizes Claisen-Schmidt condensation and an optimized process to prepare the drug candidate with fewer steps and higher yield.
An efficient new synthesis of a peroxisome proliferator-activated receptor delta agonist fonadelpar was developed. The new process features a more practical approach to construct the ethylene linker of fonadelpar by coupling an advanced aldehyde and a ketone via Claisen-Schmidt condensation, which is followed by hydrogenation and an optimized process to obtain the isoxazole moiety. The convergent synthesis provides a robust and scalable approach to prepare the drug candidate in significantly fewer steps and with a higher yield.

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