| 摘要 |
1,241,512. Spiro-heterocyclic compound. SANDOZ Ltd. 8 Jan., 1969 [24 Jan., 1968; 8 April, 1968; 29 May, 1968], No. 1136/69. Heading C2C. The invention comprises the compound of Formula (I) and its acid addition salts, and a process for making it by (a) splitting off the benzyl radical from N-benzyl-I (II), or (b) reacting benzodioxole 2-substituted by both XCH 2 and XCH 2 CH 2 (III) (wherein X is a reactive acid radical such as Br or MeS0 3 ) with NH 3 . (II) is prepared by reacting (III) with PhCH 2 NH 2 , or by reducing II-2<SP>1</SP>,5<SP>1</SP>-dione (IV) with LiAlH 4 . (III) is prepared by reacting 2-(2<SP>1</SP>-hydroxyethyl)-2-hydroxymethylbenzodioxole (V) with (e.g.) PBr 3 or MeSO 3 Cl/Et 3 N. (IV) is prepared by reacting diethyl or dimethyl 2-(benzodiorol-2-yl) succinate (VI) with PhCH 2 NH 2 , and (V) by reducing (VI) with LiAlH 4 . (VI) is made by reacting catechol with sodium and the corresponding ester of acetylenedicarboxylic or 2,2-dibromo succinic acid. Therapeutic compositions for oral and parenteral administration comprise the above compound (I), which exhibits antidepressive effects and a stimulating effect on the central nervous system. |
