| 摘要 |
<p>1,152,871. Benzofuran derivatives. ROCHE PRODUCTS Ltd. 24 April, 1967 [29 April, 1966], No. 18815/66. Heading C2C. Bacemic and optically active compounds of the general formula (R=C 1-4 alkyl, R<SP>1</SP> + R<SP>2</SP> = trimethylene, tetramethylene or butadien-(1,3)-ylene-(1,4) and X= optional Cl or Br) and their salts are prepared by reducing a compound of the formula and either reacting the resulting halohydrin with RNH 2 or converting it to the corresponding epoxide and reacting the latter with RNH 2 , optionally followed by removal of X, salt formation and/or resolution. The product of the reaction with the amine may in certain cases contain the corresponding 2-(1-alkyl. amino-2-hydroxyethyl) benzofuran as a byproduct. The starting materials II are prepared by converting a compound of the formula into an alkali metal salt, reacting the salt with chloroacetone and chlorinating or brominating the product. The compounds of the invention are #- adrenergic blocking agents and may be administered in the form of pharmaceutical preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier.</p> |
