| 摘要 |
1344720 Piperazine derivatives BOEHRINGER INGELHEIM GmbH 29 July 1971 [30 July 1970] 35772/71 Heading C2C [Also in Division A5] The invention comprises compounds of formula and their acid addition salts, wherein Ar, Ar 1 are each a fused bicyclic group (in which at least one ring is aromatic and the ring which is not directly bonded to the remainder of the molecule may be carbocyclic or heterocyclic, and saturated or aromatic, provided that Ar 1 may not be heterocyclic. In examples, these compounds are prepared by (1) introducing the ArCH 2 CH(CH 3 )- group into the (Ar 1 -substituted) piperazine; (2) forming the piperazine ring by reacting (a) a bis-chloroethylamine with the corresponding amine, or (b) a substituted ethylenediamine with ethylene dibromide or diethyl oxalate (and in the latter case reducing the thus-formed 2,3-dioxopiperazine derivatine); (3) reducing a compound of the type ArCHClCH(CH 3 )N(CH 2 CH 2 ) 2 NAr 1 . Intermediates otherwise prepared correspond with the formulae ArCH 2 CH(CH 3 )OH, ArCH 2 - CH(CH 3 )O 3 SR (R=Me or p-Ts), ArCHOHCH- (CH 3 )N(CH 2 CH 2 ) 2 NAr 1 and ArCOCH(CH 3 )N- (CH 2 CH 2 ) 2 NAr 1 . |
