| 摘要 |
NEW MATERIAL:An 10-alkyl-10-aminoalkyl-anthrone derivative of formula I: (R is alkyl group; R<1> and R<2> are H or alkyl groups; X and Y are H, halogen, alkoxy, or CF3 group; n is 1, 2 or 3), and its acid addition salt. EXAMPLE:10-Methyl-10-(2-aminoethyl)-anthrone acetate. USE:Psychotropic drugs having particularly relaxing and prolonged central nervous system stimulating and antidepressive actions, and their intermediates. PROCESS:A compound of formula II is cyanoalkylated with a cyanoalkene or a monohalonitrile to give a compound of formula III: (m is 1 or 2), which is then hydrolyzed to form a compound pf formula IV. The compound of formula IV thus obtained is subjected to the Hofmann rearrangement by the conventional method, to give a compound of formula V: (R<3> is alkyl group), which is then carboxylated and decarboxylated, and, if necessary, alkylated to afford the objective compound of formula I. |
