公开(公告)号：HUT41744A

公开(公告)日：1987-05-28

申请号：HU399986

申请日：1986-09-19

Applicant: HOECHST AG

Inventor： SIEGEL HERBERT ,  KAMPE KLAUS-DIETER ,  ALPERMANN HANS ,  GERHARDS HERMANN ,  USINGER PATRICIA ,  SCHACHT ULRICH ,  LEVEN MARGRET ,  RAETHER WOLFGANG ,  DITTMAR WALTER ,  SACHSE BURKHARD

IPC: A61K31/41 ,  A61K31/415 ,  C07D233/60 ,  C07D233/64 ,  C07D249/08 ,  C07D521/00

Abstract: Arylmethylazoles of the formula I I in which Aryl is (substituted) phenyl or naphthyl; Z is CH or N; R1 and Q are H or alkyl; R2 is H, alk(en)yl or alkynyl; R3 and R4 are H, alkyl or other hydrocarbons; or R3 and R4 together are a -(CH2)2-11 chain or a bridged -(CH2)4-5 chain, and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity. They are obtained, inter alia, from arylmethylazoles II II which are reacted with a strong base and then with a carbonyl compound III O=CR3R4; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R2Hal. If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomers are resolved.