| 摘要 |
The present invention is directed to a novel method of preparing of 2, 4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (Ha) wherein GHs CH2 Or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O-S(O)2CF3; Rg is a C1 10 alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O-S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (Ha) wherein m=0 and oxidizing the sulphur as necessary or desired.
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