发明名称 PROCEDIMIENTO PARA LA OBTENCION DE B-OXO-A-FENIL-CARBAMOIL- PIRROLPROPIONITRILOS SUSTITUIDOS
摘要 <p>For the Contracting States : DE, GB, FR, CH, LI, IT, NL, BE, SE, LU 1. A substituted beta-oxo-alpha-phenylcarbamoylpyrrolepropionitrile of the general formula I see diagramm : EP0021207,P17,F1 wherein Pl is 2- or 3-pyrrolyl substituted in the 1-position by C1 -C7 alkyl or Ph-C1 -C7 alkyl, and unsubstituted in the remaining 3 positions or substituted therein by one to three identical or different C1 -C7 alkyl groups and/or by one carboxy or C1 -C7 carbalkoxy group ; and Ph is phenyl which is unsubstituted or substituted by one to three identical or different members selected from C1 -C7 alkyl, C1 -C7 alkoxy, C1 -C7 alkylthio, hydroxy halogen, trifluoromethyl, nitro, amino or C1 -C7 alkanoylamino ; this compound in its enol form, a C1 -C7 alkyl enol ether or a C1 -C7 alkanoyl enol ester thereof, or a salt thereof with a base. For the Contracting State : AT 1. A process for the preparation of a substituted beta-oxo-alpha-phenylcarbamoylpyrrolepropionitrile of the general formula I see diagramm : EP0021207,P18,F1 wherein Pl is 2- or 3-pyrrolyl substituted in the 1-position by C1 -C7 alkyl or Ph-C1 -C7 alkyl, and unsubstituted in the remaining 3 positions or substituted therein by one to three identical or different C1 -C7 alkyl groups and/or by one carboxy or C1 -C7 carbalkoxy group ; and Ph is phenyl which is unsubstituted or substituted by one to three identical or different members selected from C1 -C7 alkyl, C1 -C7 alkoxy, C1 -C7 alkylthio, hydroxy, halogen, trifluoromethyl, nitro, amino or C1 -C7 alkanoylamino ; of this compound in its enol form, a C1 -C7 alkyl enol ether or a C1 -C7 alkanoyl enol ester thereof, or a salt thereof with a base, which process comprises a) adding compounds of formulae see diagramm : EP0021207,P18,F2 b) condensing compounds of the formulae see diagramm : EP0021207,P18,F3 and R-NH-Ph, wherein X is C1 -C7 alkoxy, C1 -C7 alkanoyloxy or halogen, or c) condensing compounds of formulae see diagramm : EP0021207,P18,F4 wherein Y is C1 -C7 alkoxycarbonyl, halocarbonyl or cyano and hydrolysing the resultant imines, or d) isomering compounds of the formula see diagramm : EP0021207,P19,F5 with a strong base and, if desired, converting a resultant compound of formula I into another compound of the invention, and/or, if desired, converting a resultant enol into a C1 -C7 alkyl enol ether or a C1 -C7 alkanoyl enol ester, and/or, if desired, converting a resultant enol into a salt with a base, or a resultant enol salt into the free enol or into another salt with a base, and/or, if desired, resolving a mixture of isomers obtained into the individual isomers.</p>
申请公布号 ES492278(D0) 申请公布日期 1981.04.01
申请号 ES19780004922 申请日期 1980.06.10
申请人 CIBA-GEIGY, AG 发明人
分类号 A61K31/40;A61P29/00;C07D207/32;C07D207/337;C07D207/34;C07D207/40;C07D207/416;C07D261/18;(IPC1-7):07D207/323;61K31/40 主分类号 A61K31/40
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