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MYOCARDIUM PROTECTING PYRROLE DERIVATIVES WITH ANTI-ARYTHMIC AND ANTI-PLATELET AGGREGATION ACTIVITY, PROCESS FOR THEIR PREPARATION AND MEDICINES CONTAINING THEM
MYOCARDIUM PROTECTING PYRROLE DERIVATIVES WITH ANTI-ARYTHMIC AND ANTI-PLATELET AGGREGATION ACTIVITY, PROCESS FOR THEIR PREPARATION AND MEDICINES CONTAINING THEM
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机译:具有抗关节炎和抗血小板凝集活性的保护心肌吡咯衍生物,其制备方法和含有它们的药物
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1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Derivatives of pyrrole of formula see diagramm : EP0054593,P16,F5 in which - R1 represents an atom of hydrogen, an alkyl group having from 1 to 6 atoms of carbon, a phenyl radical or a pyridyl-2 radical, - R2 represents an atom of hydrogen or an alkyl radical having from 1 to 6 atoms of carbon ; - R3 and R4 , which are identical or different, each represent an alkyl radical having from 1 to 6 atoms of carbon, or a cycloalkyl radical, or the group see diagramm : EP0054593,P17,F1 designates the pyrrolidinyl, piperidinyl, dimethyl-2,6 piperidinyl, morpholinyl, piperazinyl radical and the radical of formula see diagramm : EP0054593,P17,F2 - n is equal to 2 or 3, as well as the salts of these derivatives with the mineral or organic acids. 1. Claims for the Contracting State AT : Process for the preparation of derivatives of pyrrole of formula see diagramm : EP0054593,P17,F3 in which - R1 represents an atom of hydrogen, - R2 represents an atom of hydrogen or an alkyl radical having from 1 to 6 atoms of carbon, - R3 and R4 , which are identical or different, each represent an alkyl radical having from 1 to 6 atoms of carbon, or a cycloalkyl radical, or the group see diagramm : EP0054593,P17,F4 designates the pyrrolidinyl, piperidinyl, dimethyl-2,6 piperidinyl, morpholinyl, piperazinyl radical and the radical of formula see diagramm : EP0054593,P17,F5 and - n is equal to 2 or 3, as well as the salts of these derivatives with the mineral or organic acids, characterized in that the different following steps are carried out : - a compound of formula see diagramm : EP0054593,P17,F6 is used as starting product, - a saponification of the product in an alkaline medium, then a heating in an acid medium are carried out, to yield the butyric derivative of formula see diagramm : EP0054593,P18,F1 which is esterified by known processes into corresponding methyl ester, - the ester thus obtained is converted into amide by action of ammonia, - and said amide is heated with a product selected from a gamma-diketone of formula see diagramm : EP0054593,P18,F2 and dimethoxy-2,5 tetrahydrofuran, so as to form the pyrrolic cycle of the products of formula (I).
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