Synthesis

Efficient synthesis of the immunomodulating compound KRP-203

M Hamada, M Kiuchi, K Adachi

Index: Hamada, Maiko; Kiuchi, Masatoshi; Adachi, Kunitomo Synthesis, 2007 , # 13 p. 1927 - 1929

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Citation Number: 4

Abstract

Abstract A practical and concise synthesis of KRP-203 (1) was achieved by utilizing a palladium coupling reaction mediated by XantPhos and Pd 2 (dba) 3 as the key step. The coupling reaction of aryl bromide 5 with 3-hydroxythiophenol (6) proceeded chemoselectively to give phenol 7 in spite of the presence of a chlorine substituent on 5 and a hydroxyl group on 6. Phenol 7 was converted into KRP-203 by benzylation and removal ...