Tetrahedron

Syntheses of metabolites of ethyl 4-(3, 4-dimethoxyphenyl)-6, 7-dimethoxy-2-(1, 2, 4-triazol-1-ylmethyl) quinoline-3-carboxylate (TAK-603)

M Mizuno, M Yamashita, Y Sawai, K Nakamoto, M Goto

Index: Mizuno, Masahiro; Yamashita, Makoto; Sawai, Yasuhiro; Nakamoto, Koji; Goto, Mitsutaka Tetrahedron, 2006 , vol. 62, # 37 p. 8707 - 8714

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Citation Number: 8

Abstract

Convenient and efficient syntheses of ethyl 4-(3-hydroxy-4-methoxyphenyl)-6, 7-dimethoxy- 2-(1, 2, 4-triazol-1-ylmethyl) quinoline-3-carboxylate (1d) and 10-(3, 4-dimethoxyphenyl)-7, 8- dimethoxy-2H-pyridazino [4, 5-b] quinolin-1-one (1e), metabolites of TAK-603 (1), have been achieved. Use of the methanesulfonyl as a protective group of the phenolic hydroxy for Friedel–Crafts reaction enabled a new simpler synthetic route of 1d in high yield. ...