PROCESS FOR PRODUCING DERIVATIVES OF PROSTACYCLINE OR THEIR SALTS

Compounds of the formula wherein R1 is (a) hydrogen, (b) C1-10 alkyl, (c) C1-10 alkyl substituted by halogen; C1-4 alkoxy; C6-10 aryl; C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy...

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Hauptverfasser: JORGE CASALS,ES, BERND RADUECHEL,DE, GERDA MANNESMANN,DE, WERNER SKUBALLA,DE, HELMUT VORBRUEGGEN,DE, WOLFGANG LOSERT,DE
Format: Patent
Sprache:eng
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Zusammenfassung:Compounds of the formula wherein R1 is (a) hydrogen, (b) C1-10 alkyl, (c) C1-10 alkyl substituted by halogen; C1-4 alkoxy; C6-10 aryl; C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; di-C1-4-alkylamino; or tri-C1-4-alkylammonium, (d) C4-10 cycloalkyl, (e) C4-10 cycloalkyl substituted by C1-4 alkyl, (f) C6-10 aryl, (g) C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S; A is -CH2-CH2-, trans-CH=CH- or -C 3BOND C-; W is hydroxymethylene, RO-methylene, CH3 or CH3, wherein OH or OR is in the alpha - or beta -position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins; D and E together are a direct bond, or D is C1-10 alkylene, C1-10 alkenylene or C1-10 alkynylene or one of these groups substituted by fluorine, and E is oxygen, -C 3BOND C- or a direct bond; R2 is (a) a C1-10 hydrocarbon aliphatic radical, (b) a C6-10 hydrocarbon aliphatic radical substituted by C6-10 aryl or by C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; (c) C4-10 cycloalkyl, (d) C4-10 cycloalkyl substituted by C1-4 alkyl, (e) C6-10 aryl, (f) C6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C1-4 alkoxy group; or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S; and R3 is OH or OR; and, when R1 is hydrogen, the salts thereof with physiologically compatible bases, are effective as antihypertensive, bronchiodilators, thrombocyte aggregation inhibitors, inter alia.