Process development of a disease-modifying antirheumatic drug, TAK-603, based on optimization of Friedel-Crafts reaction and selective substitution of a triazole ring |
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| Authors: | Masahiro Mizuno Atsushi Inagaki Makoto Yamashita Norie Soma Yoshiharu Maeda Hiroshi Nakatani |
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| Institution: | Chemical Development Laboratories, Pharmaceutical Production Division, Takeda Pharmaceutical Company Limited, 17-85, Jusohonmachi 2-chome, Yodogawa-ku, Osaka 532-8686, Japan |
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| Abstract: | A practical method for the preparation of TAK-603, 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 TAK-603, 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. |
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| Keywords: | TAK-603 Friedel-Crafts reaction Selective substitution 1 2 4-Triazole |
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