| 摘要 |
1. Claims for the contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE Carbacyclin derivatives of the general formula I see diagramm : EP0057660,P15,F5 wherein R1 is the group OR2 , where R2 is hydrogen or alkyl of 1-4 carbon atoms, or the group NHR3 , where R3 is acetyl, methanesulfonyl or hydrogen, W is a hydroxymethylene group or a see diagramm : EP0057660,P15,F6 group, in which the OH is in the alpha- or beta-configuration, D is a straight or branched chain alkylene group of 1-5 carbon atoms, R4 is alkyl of 1-7 carbon atoms, and when R2 is hydrogen, salts of these compounds with physiologically acceptable bases. 1. Claim for the contracting State : AT Process for the preparation of the carbacyclin derivatives of the general formula I see diagramm : EP0057660,P17,F1 wherein R1 is the group OR2 , where R2 is hydrogen or alkyl of 1-4 carbon atoms, or the group NHR3 , where R3 is acetyl, methanesulfonyl or hydrogen, W is a hydroxymethylene group or a see diagramm : EP0057660,P17,F2 group, in which the OH is in the alpha- or beta-configuration, D is a straight or branched chain alkylene group of 1-5 carbon atoms, R4 is alkyl of 1-7 carbon atoms, and when R2 is hydrogen, salts of these compounds with physiologically acceptable bases, characterised in that a double bond is introduced in known manner in the 2-position into a compound of general formula II see diagramm : EP0057660,P17,F3 by reacting it with a lithium alkylamine of general formula III see diagramm : EP0057660,P18,F1 wherein R8 and R9 are alkyl of 1-10 carbon atoms, cycloalkyl of 3-6 carbon atoms or a trialkylsilyl group in which the alkyl is of 1-4 carbon atoms, treating it with a phenyl compound of general formula IV see diagramm : EP0057660,P18,F2 in which R10 is the group see diagramm : EP0057660,P18,F3 see diagramm : EP0057660,P18,F4 or -Se-Br and oxidising it, and then optionally, and in an arbitrary sequence separating the isomers, and/or freeing protected hydroxy groups, and/or esterifying or etherifying free hydroxy groups, and/or esterifying a free carboxyl group and/or saponifying an esterified carboxyl group or converting a carboxyl group into a -CONHR3 group or into a salt with a physiologically acceptable base. |
