Practical Synthesis of 4??Fluoro??2??(methylthio) benzylamine and the Corresponding Sulfone and Sulfonamide

…, MS Kuo, HM Moritz, JS Wai, MS Egbertson

Index: Perlow, Debra S.; Kuo, Michelle S.; Moritz, H. Marie; Wai, John S.; Egbertson, Melissa S. Synthetic Communications, 2007 , vol. 37, # 11 p. 1887 - 1897

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Citation Number: 5

Abstract

Abstract Practical syntheses of 4??fluoro??2??(methylthio) benzylamine 1 and the corresponding 2??methylsulfonyl analog 2 are reported. The methylthio moiety was introduced regioselectively by two methods. In the first method, metallation of 4??fluoro??2?? bromobenzoic acid, followed by treatment with dimethyl disulfide resulted in an easily isolated intermediate, which was suitable for further elaboration to the benzylamine 1. In ...