rel-(2R,6S)-2,6-Dimethylpiperidine → 4-Chloro-6-(cis-2,6-dimethylpiperidino)-5-fluoropyrimidine

反応式

Cl[C:2]1[C:7]([F:8])=[C:6]([Cl:9])[N:5]=[CH:4][N:3]=1.[CH3:10][C@H:11]1[CH2:16][CH2:15][CH2:14][C@@H:13]([CH3:17])[NH:12]1>>[Cl:9][C:6]1[C:7]([F:8])=[C:2]([N:12]2[C@H:13]([CH3:17])[CH2:14][CH2:15][CH2:16][C@@H:11]2[CH3:10])[N:3]=[CH:4][N:5]=1

参加物

反応物 2

HCID 641768rel-(2R,6S)-2,6-Dimethylpiperidine

HCID 112866754,6-Dichloro-5-fluoropyrimidine

生成物 1

HCID 866074674-Chloro-6-(cis-2,6-dimethylpiperidino)-5-fluoropyrimidine収率 57.5%

反応条件

温度: 70 °C

実験手順

0.25 g of 4,6-dichloro-5-fluoropyrimidine and 0.34 g of cis-2,6-dimethylpiperidine were mixed and stirred for 11 hours at 70° C. The reaction mixture was subjected to silica gel column chromatography to obtain 0.21 g of 4-chloro-6-(cis-2,6-dimethylpiperidino)-5-fluoropyrimidine.