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摘要
A new synthetic approach to elvucitabine started from L-xylose via the reactions of 10 steps in an overall yield of 20% was developed. The key steps included trimethylsilyl trifluoromethanesulfonate(TMSOTf)-mediated stereocontrolled beta-glycosidation and exquisite choice of chloroacetyl group for the protection of hydroxyl groups as well as the corresponding deprotection under notably mild conditions. The structure of elvucitabine, in particular, the stereochemistry thereof, was unambiguously determined by comparison of the physical properties, such as H-1 NMR data and the specific rotation, of the synthesized sample with those reported.
- 出版日期2013-2
- 单位天津药物研究院有限公司
