| 摘要 |
<p>1,170,280. N-Naphthylamino acid derivatives. PHILIPS' GLOEILAMPENFABRIEKEN N.V. 30 Nov., 1966 [30 Nov., 1965], No. 53558/66. Heading C2C. Novel compounds of general Formula I in which R 1 represents hydrogen or a metal atom, for example, sodium or potassium, or an alkyl group, R 2 represents a branched or straight-chain alkylene group comprising altogether from 3 to 7 carbon atoms, not being a substituted methylene group, and R 3 represents hydrogen, a halogen atom, for example, chlorine or bromine, or an alkoxy group having 1 to 4 carbon atoms or acid-addition salts of the said compounds formed with pharmaceuticallyacceptable acids are prepared by various methods (a) by reacting a naphthylamine of Formula II with a compound wherein R<SP>1</SP> 2 is an alkenyl group; (b) a compound of Formula II is reacted with a compound O = R<SP>11</SP> 2 -COOR<SP>1</SP> followed by catalytic reduction of the intermediately formed Schiffs base, R<SP>11</SP> 2 is a hydrocarbon residue convertible to R 2 during the reduction; (c) a nitrile is hydrolyzed to give the above compounds wherein R 1 is H and the carboxyl group may be then esterified to obtain a compound of Formula I in which R 1 represents an alkyl group; (d) an amine of Formula II is reacted with (e) an amine of Formula II is reacted with a lactone and the resulting free acid is optionally esterified; (f) a halogen compound of is reacted with H 2 N-R 2 -COOR 1 except where R 3 in Formula I is halogen; in all cases the reaction may be followed by salt formation or interconversion. Pharmaceutical compositions having sedative action and being in conventional forms for oral, rectal or parenteral administration comprise an above novel compound or a salt thereof and a carrier therefor.</p> |
