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Convenient synthesis of 2-(methylsulfonyl)pyrimidine derivatives
Authors:Tong-Hui Huang  Shan-Shan Zhou  Xin Wu  Lin An
Affiliation:Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, School of Pharmacy, Xuzhou Medical University, Xuzhou, China
Abstract:An efficient and convenient approach for the preparation of functionalized 2-(methylsulfonyl)pyrimidine derivatives has been developed through cyclic condensation of malonate derivatives with S-methylisothiouronium sulfate followed by derivation and oxidation in water–acetone mixture using oxone as the oxidant. This synthetic strategy provides an efficient and environmentally friendly approach for easy access to 2-(methylsulfonyl)pyrimidine derivatives with considerable yields.
Keywords:2-(Methylsulfonyl)pyrimidine  2-(methylthio)pyrimidine  cyclization  oxidation
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