p-Toluenesulfonate → 1-(4-((2-(Hydroxymethyl)benzyl)(methyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)ethanone

反応式

[CH3:1][NH:2][CH2:3][C:4]1[CH:9]=[CH:8][CH:7]=[CH:6][C:5]=1[CH2:10][OH:11].FC(F)(F)S(O[C:18]1[C:19]2[CH2:39][N:38]([C:40](=[O:42])[CH3:41])[CH2:37][CH2:36][C:20]=2[N:21]=[C:22]([NH:24][C:25]2[CH:30]=[CH:29][C:28]([C:31]3[O:35][CH:34]=[N:33][CH:32]=3)=[CH:27][CH:26]=2)[N:23]=1)(=O)=O.S(C1C=CC(C)=CC=1)([O-])(=O)=O>>[OH:11][CH2:10][C:5]1[CH:6]=[CH:7][CH:8]=[CH:9][C:4]=1[CH2:3][N:2]([CH3:1])[C:18]1[C:19]2[CH2:39][N:38]([C:40](=[O:42])[CH3:41])[CH2:37][CH2:36][C:20]=2[N:21]=[C:22]([NH:24][C:25]2[CH:30]=[CH:29][C:28]([C:31]3[O:35][CH:34]=[N:33][CH:32]=3)=[CH:27][CH:26]=2)[N:23]=1

参加物

反応物 3

HCID 85570p-Toluenesulfonate

HCID 21825614HCID 21825614、化合物

HCID 593337606-Acetyl-2-(4-(oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl trifluoromethanesulfonate

生成物 1

HCID 462000541-(4-((2-(Hydroxymethyl)benzyl)(methyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)ethanone収率 15.3%

実験手順

1-(4-((2-(Hydroxymethyl)benzyl)(methyl)amino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)ethanone (12.3 mg, 15.3%) was prepared from (2-((methylamino)methyl)phenyl)methanol and 6-acetyl-2-(4-(oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-y1 trifluoromethanesulfonate (example 88a) according to the general procedure for amine substitution of tosylate on pyrimidines.