| 摘要 |
1465783 Pyrroles CIBA-GEIGY AG 7 March 1974 [9 March 1973 1 Feb 1974] 10223/74 Heading C2C Compounds of the general formula (Py = optionally alkylated 1-pyrrolyl; Ph = phenylene; R 1 =H, alkyl; R 2 =H, alkyl, arylalkyl, optionally functionally modified carboxyalkyl; or R 1+2 =alkylene, oxa-alkylene, thiaalkylene, optionally substituted aza-alkylene) and their salts are prepared by standard methods, such as (a) reacting a compound of the formula Py-PhOCH 2 CH(X 1 )CH 2 Z 1 with Z 2 R 1 or Z 2 R 2 (one of Z 1,2 is NHR 2 or NHR 1 and the other is a reactive ester residue and X 1 is OH or, if Z 2 is NHR 2 or NHR 1 , Z 1 +X 1 is -O-, provided that Z 1 is not NH 2 ) or (b) reacting a compound of the formula H 2 NPhOCH 2 CHOHCH 2 NR 1 R 2 with aγ-oxo-alkanone or tautomer or functional derivative thereof, optionally followed by salt formation. The preparation of oxiranyl starting materials for process (a) and the corresponding pyrrolylphenols, and starting materials for process (b) is described. The above compounds are #-adrenergic blocking agents, and may be administered in the form of pharmaceutical and veterinary preparations containing them in association with a carrier.
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