| 摘要 |
Pyrimidine derivs. of formula (I) are new. In (I) NR2R3 is (a) azcridimyl and R, R1=NH2, OCH3, (b) NH (CH2)2NR4R5, (c) U-Q'-pyrrolidin-3-yl)amino, Q' is cyclohexyl and R, R1 as in (a), or Q' is benzyl or 4-fluorobenzyl and R R1 are CH3OCH3 or NH2, OCH3, (d) 1-benzyl-piperidin-4-yl and R, R1 are Z, OCH3, or NH2, OCH7-iso (Z is NH2, CH3, H, CH3O, (CH3)2N or CH3NH), (e) racemic (1-R10-pyrrolidin-2-yl) amino, R10 is CH3 and R, R1 are NH2. OCH3, CH3, OCH3, CH3, EOt, or Et, OEt, or R10 is Et and R, R1 are Z, OCH3, NH2, Z1 (Z1 is ErO, n - or iso-C3H7O), CH3, Z1, Et, OEt, n- or is o-C3H7, OCH3, CH3S, OCH3, or R10 is n-propyl, n-butyl, benzyl or p-fluorobenzyl and R, R1 are NH2, OCH3 or CH3, OCH3, or CH3, OCH3, or R10 is cyclohexylmethyl or allyl and R, R1 are CH3, OCH3. In (I), NR2R3 is (f) the gp. R, R1 are CH3, OCH3 CH3, OEt, (CH3)2N, OCH3 or (CH3)2N, OEt, (g) (1-methylpyrrol-2-yl)methylamino and R1R1 are CH3, OCH3. In (b) NR4R5 is (d) 1,2,3,4-tetrahydroquinoline gp. or anilino and R, R1 are R, R1 =NH2, OCH3, NH2, OEt, CH3, OCH3, CH3S, OCH3 or (CH3)2N, OCH3, (iii)-N(R6) R6, R7 are CH3, H and R, R1=NH2, OCH3, R6, R7 Et, H and R, R1 are NH2, OCH3, CH3, OCH3 or CH3, OEt, or R6R7 are Et, F and R, R1 are CH3, OCH3 or CH3, OEt, (iv) 4-Q-piperazino, Q is phenyl or 4-fluorophenyl and R, R1 are CH3, OCH3, or Q is 2-methoxyphenyl and R, R1 are CH3, OCH3 or NH2, OCH3. (I) are neuroleptics useful for treating psychic disorders. The cpd. with R, R1 = NH2, OCHo and NR2R3-2-(diethylamino) ethylamine has intraperitoneal LD50 in mice 650 mg/kg. |
