Synthesis of Related Substances of Alogliptin Benzoate
In this article,based on the industrial synthetic route of alogliptin benzoate(1),seven related substances of 1 were synthesized,namely 2,2'-[[6-chloro-3-methyl-2,4-dioxo-3,4-dihydropyrimidine-1,5(2H)-diyl]-bis(methylene)]-dibenzonitrile(7),2-[[5-bromo-6-chloro-3-methyl-2,4-dioxo-3,4-dihydropyrimidine-1(2H)-yl]-methyl]benzonitrile(8),2,2'-[[6-ethoxy-3-methyl-2,4-dioxo-3,4-dihydropyrimidine-1,5(2H)-diyl]bis(methylene)]-dibenzonitrile(9),(R)-2-[[3-methyl-2,4-dioxo-6-[(piperidin-3-yl)amino]-3,4-dihydropyrimidine-1(2H)-yl]methyl]-benzonitrile(10),(R)-2-[[6-[3-[[3-(2-cyanobenzyl)-1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl]amino]-piperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidine-1(2H)-yl]methyl]benzonitrile(11),(R)-2-[[3-methyl-6-[3-[(1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-yl)amino]piperidin-1-yl]-2,4-dioxo-3,4-dihydropyrimidine-1(2H)-yl]methyl]benzonitrile(12),(R)-N-[1-[3-(2-cyanobenzyl)-1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-yl]piperidin-3-yl]benzamide(13).Their structures were confirmed by 1H NMR,13C NMR and MS.The synthesis of 7,9,12,and 13 were reported at the first time.
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