Zhu Yizhong, Zhang Xiquan, L. Fei
Nov 2, 2015
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Journal
Chinese Journal of Applied Chemistry
Abstract
Tedizolid with a yield of 82. 9% was synthesized by the Suzuki coupling reaction of 5-bromo-2-( 2-methyl-2H-tetrazol-5-yl) pyridine and( 5R)-3-( 4-bromo-3-fluorophenyl)-5-( hydroxymethyl)-2-oxazolidinone which was prepared from bis( pinacolato) diboron using 1,1'-bis( diphenylphosphino) ferrocene-palladium( Ⅱ)dichloride dichloromethane complex as the catalyst. The effect of the catalytic system on the reaction of the borylation reaction and Suzuki reaction was investigated respectively,and the optimum reaction conditions were determined. Tedizolid phosphate was obtained by reaction of tedizolid with dibenzyl N, Ndiisopropylphosphoramidite,and subsequent debenzylation with Pd / C. The total yield is 66. 2%.