Process development of a disease-modifying antirheumatic drug, TAK-603, based on optimization of Friedel–Crafts reaction and selective substitution of a triazole ring

M Mizuno, A Inagaki, M Yamashita, N Soma, Y Maeda…

Index: Mizuno, Masahiro; Inagaki, Atsushi; Yamashita, Makoto; Soma, Norie; Maeda, Yoshiharu; Nakatani, Hiroshi Tetrahedron, 2006 , vol. 62, # 17 p. 4065 - 4070

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Citation Number: 15

Abstract

A practical method for the preparation of, an antirheumatic drug, has been developed. As a result of optimizing the Friedel–Crafts reaction in the presence of SnCl4/POCl3, 2- aminobenzophenone skeleton, the key intermediate of, was formed with good yield. The selective substitution reaction of 1, 2, 4-triazole was accomplished using 4-amino-1, 2, 4- triazole and deamination.