(S)-(+)-2-(Aminomethyl)pyrrolidine → HCID 178508759, 화합물

HRID 1665089노트

반응식

HRID 1665089 반응식
[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

참가 물질

4

반응물 2

HCID 2734054(S)-(+)-2-(Aminomethyl)pyrrolidineHCID 1404443183,5-Diamino-6-chloro-N-[(methylsulfanyl)methanimidoyl]pyrazine-2-carboxamide2회

생성물 1

HCID 178508759HCID 178508759, 화합물

시약·촉매·용매 1

HCID 3776Isopropanol용매

반응 조건

온도
60 °C

실험 절차

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

후처리

  1. temperatureto cool to room temperature
  2. customthe precipitate is removed by filtration
  3. concentrationThe filtrate is concentrated in vacuo
  4. customthe residue purified by chromatography (SiO2, DCM/MeOH)

출처 및 근거

ORD 기록
ord-180485e272ce4b2cb653f4b5c0f1476b
출처 데이터셋
uspto-grants-2011_10
특허 번호
US08039472B2

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