| 主权项 |
1. A method of making a compound of formula (I):comprising allowing a compound of formula (II):to react in the presence of base to form the compound of formula (I), wherein:
m and n are each independently 0, 1 or 2; R1 is a leaving group selected from chloro, bromo, iodo, methoxy, arylsulfonyloxy and trifluoromethanesulfonyloxy; or R1 is a carbocyclic or heterocyclic ring selected from phenyl, thienyl, pyridyl, N-oxo-pyridyl, cyclopropyl, piperidinyl, piperazinyl, morpholinyl, thiazolyl, oxadiazolyl, thiadiazolyl, pyrazolyl, S,S-dioxothiazinyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benztriazolyl, oxodihydropyridyl, oxodihydropyridazinyl, oxodihydropyrimidinyl and oxodihydropyrazinyl; wherein each of the foregoing R1 carbocyclic or heterocyclic rings may be optionally substituted by 1 to 4 groups; wherein substituents for ring carbon atoms of said carbocyclic or heterocyclic rings are independently selected from halogen, cyano, oxo, nitro, —(C1-C6)alkyl, —O(C1-C6)alkyl, and —(C3-C6)cycloalkyl; and wherein substituents for ring nitrogen atoms of said heterocyclic rings, when present, are selected from —(C1-C6)alkyl and —(C3-C6)cycloalkyl; each R2 and R3 is independently selected from —(C1-C6)alkyl, —O(C1-C6)alkyl, and —(C3-C6)cycloalkyl; wherein each of the —(C1-C6)alkyl, —O(C1-C6)alkyl, and —(C3-C6)cycloalkyl of said R2 and R3 is optionally independently substituted with one to three R6 groups; R4 is selected from —(C1-C6)alkyl and —(C3-C6)cycloalkyl; wherein the —(C1-C6)alkyl and —(C3-C6)cycloalkyl of said R4 is optionally substituted with one to three R6 groups; R5 is selected from —(C1-C6)alkyl, —(C3-C6)cycloalkyl, and phenyl; and each R6 is independently selected from halo, —(C1-C6)alkyl, —O(C1-C6)alkyl, and —(C3-C6)cycloalkyl. |
