An Improved Preparation Process for Gemcitabine

An improved, cost-effective, and convenient process, using cinnamoyl as hydroxyl protective group and tosyl as the leaving group for gemcitabine (1) is described. The overall yield obtained from this newly developed process is around 10%, including two stereospecific crystallizations, and the qualit...

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Veröffentlicht in:Organic process research & development 2008-09, Vol.12 (5), p.888-891
Hauptverfasser: Jiang, Xiangrui, Li, Jianfeng, Zhang, Rongxia, Zhu, Yi, Shen, Jingshan
Format: Artikel
Sprache:eng
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Zusammenfassung:An improved, cost-effective, and convenient process, using cinnamoyl as hydroxyl protective group and tosyl as the leaving group for gemcitabine (1) is described. The overall yield obtained from this newly developed process is around 10%, including two stereospecific crystallizations, and the quality of the product complies with the requirements of USP30.
ISSN:1083-6160
1520-586X
DOI:10.1021/op800104r