(S)-(+)-2-(Aminomethyl)pyrrolidine → HCID 178508759、化合物
反応式
[NH2:1][C:2]1[C:3]([C:10]([NH:12][C:13](=[NH:16])SC)=[O:11])=[N:4][C:5]([Cl:9])=[C:6]([NH2:8])[N:7]=1.[NH2:17][CH2:18][C@@H:19]1[CH2:23][CH2:22][CH2:21]N1>CC(O)C>[NH2:1][C:2]1[C:3]([C:10]([N:12]=[C:13]2[N:16]3[CH2:21][CH2:22][CH2:23][CH:19]3[CH2:18][NH:17]2)=[O:11])=[N:4][C:5]([Cl:9])=[C:6]([NH2:8])[N:7]=1参加物
4
反応条件
- 温度
- 60 °C
実験手順
1-(3,5-Diamino-6-chloro-pyrazine-2-carbonyl)-2-methyl-isothiourea (Intermediate A) (195 mg, 0.5 mmol) is suspended in propan-2-ol (10 ml) and (S)-2-(aminomethyl)pyrrolidine (100 mg, 1 mmol) is added. The mixture is heated at 60° C. for 18 hours, allowed to cool to room temperature and the precipitate is removed by filtration. The filtrate is concentrated in vacuo and the residue purified by chromatography (SiO2, DCM/MeOH) to afford the title compound as a light, yellow gum; [M+H]+ 296