C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/311, 260/314
C07D 233/54 (2006.01) A61K 31/415 (2006.01) C07D 233/64 (2006.01) C07D 233/66 (2006.01) C07D 263/30 (2006.01) C07D 263/32 (2006.01) C07D 277/20 (2006.01) C07D 277/22 (2006.01)
Patent
CA 1187088
ABSTRACT A method of producing a 3,5-di-tert-butyl-4-hydroxyphenyl- substituted heterocyclic compound represented by formula I Image wherein one of R1, R2, and R3 represents a 3,5-di-tert-butyl-4- hydroxyphenyl group Image and others represent a hydrogen atom, a lower alkyl group, a lower aralkyl group, an aryl group, a lower alkoxy-substituted aryl group, or the group shown by -O-Z, Image , or -NH-Z (wherein Z represents a hydrogen atom, a lower alkyl group, a carboxy lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower aralkyl group, or a aryl group and n represents 0, 1, or 2) and A represents an oxy- gen atom, a sulfur atom, an imino group, a lower alkylimino group, or a 3,5-di-tert-butyl-4-hydroxyphenacylimino group Image Image or a salt thereof which comprises reacting the compound repre- sented by formula II Image II and the ?-halocarbonyl compound represented by formula III Image III ABSTRACT: wherein R1, R2, R3, and A have the same significance as defined concerning formula I; A' represents an oxygen atom, a sulfur atom, an imino group, or a lower alkylimino group; and X repre- sents a halogen atom; and then, if desired, oxidizing, alkylat- ing or desulfurizing the product thus obtained. The compounds of this invention have an anti-inflammatory, an antipyretic, an analgesic, an anti-arthritic activity, and an immuno regulatory activity. Hence, they are particularly useful as an antirheumatic.
396507
Homma Hiroshige
Isomura Yasuo
Kubo Kazuo
Sakamoto Shuichi
Johnson Douglas S. Q.c.
Yamanouchi Pharmaceutical Co. Ltd.
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