| 摘要 |
<p>1,154,193. Salts of meta- or para-substituted phenylethanolalkylamines. P. PRATESI, L. VILLA and E. GANA. 10 July, 1967 [14 July, 1966], No. 31611/67. Heading C2C. Novel salts suitable as stimulating and inhibiting agents for beta-adrenergic receptors of the general formula wherein Z is a hydrogen atom and Y is -CN, -CF 3 , -SCH 3 , or -COOCH 3 , or, Y is a hydrogen atom and Z is -CN, -CF 3 , or -SCH 3 , R is a C 3 or C 4 alkyl radical and X is Cl<SP>-</SP>, Br<SP>-</SP>, SO<SP>=</SP> 4 , PO<SP>#</SP> 4 , CH 3 COO-or COOH(CHOH) 2 COO- are prepared: (a) by reducing a phenacyl compound of the formula wherein G is a chlorine or bromine atom with NaBH 4 , condensing the resulting product with a C 3 or C 4 alkylamine followed by salification with the appropriate acid; (b) by condensing the above phenacyl compound with the alkylamine and subsequently reducing and salifying with NaBH 4 or hydrogen, and (c) by reducing the condensation product between a Y, Z-substituted phenyl-glyoxal and an alkylamine and salifying with an acid. 2 - Bromo - 1 - (p - trifluoromethylphenyl) - ethanol, 2 - bromo - and 2 - chloro - 1 - (m - cyano - phenyl) - ethanol, 2 - bromo - 1 - (p - methylthio - phenyl) - ethanol and 2 - bromo - 1 - (p - methoxycarbonylphenyl) - ethanol are obtained by reduction of the corresponding phenacyl halide. Omega - isopropylamino - 4 - methylthio - acetophenone (and the hydrochloride thereof) is obtained by the interaction of isopropylamine and 4 - methylthio - phenacyl bromide. Omega - isopropylamino - 4 methoxycarbonyl - acetophenone (and the hydrochloride thereof) is obtained similarly.</p> |
