Bicyclic derivative 3-o4-derivative 4-substitute 4 - (amino acid) - pyridine, preparation procedure, drug synthesis containing these derivatives, preparation procedure, compound intermediate and preparation procedure.

摘要

The dicycloaniline of a 3-o-4, 4 - (amino) derivative, including (I) a stereochemical derivative form, a nitrous oxide form, or a basic addictive salt or an acceptable pharmacological acid, in which R1 and R2 together constitute a distinct radical substance Formula - o-ch2-o - (A-1),-O-CH2-CH2- (a-2),-O-CH2-CH2-O-3-O-CH2-CH2-CH2- (a-4), - O-CH2-CH2-CH2-O- (a5),-O-CH2-CH2-CH2-CH2- (a6) where in said divalent radicals one or two hydrogen atoms can be substituted with C1-6alkyl R3 is hydrogen or halo; R4 is hydrogen or C1-6 alkyl, R5 is hydrogen or C1-6 alkyl, L is C3-6 cycloalkyl C5-8 cycloalkanone or C2-6 alkenyl or L is a radical of the formula -Alk-R6 (b-1) ,-Alk-X-R7 (b-2)-Alk-Y-C (3DO) -R9 (b-3)o -Alk-Y-C (3DO) -NR11R12 (b4)where each Alk is C1-2 alkanediyl; and R6 is hydrogen, hydroxy, cyano, C1-6 alkylsulfonylamino, C3-6 cycloalkyl, cycloalcanone C5-6 or Het1; R7 is hydrogen, C1-6 alkyl, hydroxyalkyl C1-6, cycloalkyl C3-6, or Het 2, X is O, S, SO2 or NR8, said R8 being hydrogen or C1-6 alkyl, R9 is hydrogen, C1- alkyl 6, C3-6cycloalkyl, C1-6alkyloxy, hydroxy; Y is N R10 or a direct bond, said R10 being hydrogen or C1-6 alkyl, R11 and R12 are each independently hydrogen,C1-6cycle-quilo C3-6 or R11 and R12, together with the nitrogen atoms carrying R11 and R12, can form a nillo of pirrolidini or piperidinilo and ambospueden, which can be replaced by C1-6 amino or di (C1-6 tar) amino or R11 and R12 combined with the nitro containing de11 and R12. The nontoxic pyridine or 4-morphine alcohol can be replaced by C1-6 tar, and het1 and het2 are 1 respectively.