| 摘要 |
1457715 Aminoalkoxybenzoyl-benzofurans and -benzothiophenes; organocopper compounds SMITHKLINE CORP 19 June 1975 [20 June 1974] 26069/75 Headings C2C and C2J [Also in Division C5] The invention comprises compounds of formula and their pharmaceutically acceptable acid addition salts, wherein R 1 is H, Br, Cl, F, CF 3 , NO 2 or C 1-4 alkyl or alkoxy; R 2 and R 3 are each H or C 1-4 alkyl or alkoxy; R 4 and R 5 are each Me, Et, Pr or Bu, or R 4 may be H; R 6 is Ph (optionally substituted by CF 3 or by up to 3 of Br, Cl, F or C 1-4 alkyl or alkoxy) or PhCH 2 (optionally ring-substituted by Br, Cl, F, CF 3 or C 1-4 alkyl or alkoxy); n is 2-4; and Z is O or S. In examples, these compounds are prepared by (a) a Friedel-Crafts acylation of the corresponding (R 1 +R 6 -substituted) benzofuran or benzothiophene, using the chloride of an aminoalkoxybenzoic acid; (b) etherification of the corresponding hydroxybenzoyl benzofuran; or (c) amination of the bromoalkoxy benzoylbenzofuran. Starting materials and intermediates otherwise prepared are those of formulµ PhCH : CBr 2 , PhC : CH and PhC : CCu, in which Ph is substituted as indicated above for R 6 ; substituted 2-benzoylfurans and their hydrazones; methoxybenzoylbenzofurans; R 2 and R 3 substituted methoxy- and hydroxybenzoic acids and their methyl esters and acid chlorides; substituted alpha-phenoxyacetophenones; and m-BrCH 2 COC 6 H 4 CF 3 . Therapeutic compositions having coronary vasodilator and hypotensive activity comprise compounds of the above formula, and may be administered orally or parenterally.
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