To obtain a new compound having potent α1 blocking action and serotonin-2 receptor antagonism, low in both toxicity and side effect, thus useful as a medicine for preventing/treating circulatory diseases such as hypertension and cardiac failure.
This compound is expressed by formula I {ring P is a pyrrole ring of formula II [A is an alkylene, alkenylene, etc.; Y is a group of formula III (W is CH, C=, etc.; B is O, S, carbonyl, etc.; (m) is 0 or 1; E1 and E2 are each H a lower alkyl; D is a (substituted) aromatic hydrocarbon group, etc.)]; dotted line indicates the presence or absence of a bond; Z1 and Z2 are each H, O, etc.; R is H, an alkyl, etc.}, e.g. benzyl-3-(3-pyrrolecarboxamido)propionate. The compound of formula I is obtained by the following process: a compound of formula IV is treated with e.g. an inorganic salt and then reacted with a compound of the formula X-A-X' (X and X' are each an eliminable group) at 20°C to the reflux temperature to effect conversion to a compound of formula V, which in turn is reacted with an N2-contg. compound of the formula H-Y at room temperature to 150°C in the presence of an alkali iodide together with, as necessary, an organic base such as triethylamine.
SHIBATA MAKOTO
IWAMORI CHIE
INOMATA NORIO
