Access to chiral phthalidyl ester prodrugs via an isothiourea-catalyzed dynamic kinetic resolution reaction.

IF 2.9 3区化学 Q1 CHEMISTRY, ORGANIC

Organic & Biomolecular Chemistry Pub Date : 2025-03-25 DOI:10.1039/d4ob02057j

Hui Cai, Chaoyang Song, Dan Ling, Youlin Deng, Zhichao Jin, Tingting Li

引用次数: 0

Abstract

An isothiourea-catalyzed acylative dynamic kinetic resolution reaction has been developed for the synthesis of chiral phthalidyl ester prodrugs. Various chiral phthalidyl esters were obtained in moderate to excellent yields (up to 97%) and good to excellent optical purities (up to 99 : 1 er). Notably, a variety of acyl chlorides were well tolerated, even those derived from pharmaceuticals, agrochemicals, and natural products. This catalytic transformation is an effective strategy for the development of chiral phthalidyl ester prodrugs.

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来源期刊

Organic & Biomolecular Chemistry 化学-有机化学

CiteScore

5.50

自引率

9.40%

发文量

1056

审稿时长

1.3 months

期刊介绍： Organic & Biomolecular Chemistry is an international journal using integrated research in chemistry-organic chemistry. Founded in 2003 by the Royal Society of Chemistry, the journal is published in Semimonthly issues and has been indexed by SCIE, a leading international database. The journal focuses on the key research and cutting-edge progress in the field of chemistry-organic chemistry, publishes and reports the research results in this field in a timely manner, and is committed to becoming a window and platform for rapid academic exchanges among peers in this field. The journal's impact factor in 2023 is 2.9, and its CiteScore is 5.5.