Hydrochloric Acid → (S)-1-((R)-2,2,2-trifluoro-1-(3-(8-((R)-1-methoxypropan-2-yloxy)quinolin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)ethyl)pyrrolidin-3-amine dihydrochloride

HRID 338958노트

반응식

HRID 338958 반응식
[F:1][C:2]([F:43])([F:42])[C@H:3]([N:29]1[CH2:33][CH2:32][C@H:31]([NH:34]C(=O)OC(C)(C)C)[CH2:30]1)[C:4]1[CH:5]=[CH:6][C:7]2[N:8]([C:10]([C:13]3[CH:22]=[CH:21][C:20]4[C:15](=[C:16]([O:23][C@H:24]([CH3:28])[CH2:25][O:26][CH3:27])[CH:17]=[CH:18][CH:19]=4)[N:14]=3)=[N:11][N:12]=2)[CH:9]=1.[ClH:44]>ClCCl>[ClH:44].[ClH:44].[F:42][C:2]([F:1])([F:43])[C@H:3]([N:29]1[CH2:33][CH2:32][C@H:31]([NH2:34])[CH2:30]1)[C:4]1[CH:5]=[CH:6][C:7]2[N:8]([C:10]([C:13]3[CH:22]=[CH:21][C:20]4[C:15](=[C:16]([O:23][C@H:24]([CH3:28])[CH2:25][O:26][CH3:27])[CH:17]=[CH:18][CH:19]=4)[N:14]=3)=[N:11][N:12]=2)[CH:9]=1

참가 물질

4

반응물 2

HCID 313Hydrochloric AcidHCID 86707476tert-butyl (S)-1-((R)-2,2,2-trifluoro-1-(3-(8-((R)-1-methoxypropan-2-yloxy)quinolin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)ethyl)pyrrolidin-3-ylcarbamate

생성물 1

HCID 86707477(S)-1-((R)-2,2,2-trifluoro-1-(3-(8-((R)-1-methoxypropan-2-yloxy)quinolin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)ethyl)pyrrolidin-3-amine dihydrochloride수율 177.2%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

To a solution of tert-butyl (S)-1-((R)-2,2,2-trifluoro-1-(3-(8-((R)-1-methoxypropan-2-yloxy)quinolin-2-yl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)ethyl)pyrrolidin-3-ylcarbamate (0.37 g, 0.61 mmol) in dichloromethane (1 mL) was added hydrochloric acid (5-6M in 2-propanol; 8.7 mL, 0.61 mmol). The reaction mixture was stirred at ambient temperature for 30 minutes. The solvent was removed under reduced pressure, and the resulting solid was suspended in acetonitrile (3 mL) and stirred at ambient temperature for 5 minutes. The solid was collected by vacuum filtration to give the title compound (0.31 g, 87%). LCMS APCI (+) m/z 501 (M+H). Specific rotation: [α]25D=0.48° (c=1.03, MeOH).

후처리

  1. customThe solvent was removed under reduced pressure
  2. stirringstirred at ambient temperature for 5 minutes
  3. filtrationThe solid was collected by vacuum filtration

출처 및 근거

ORD 기록
ord-bd7855df3e4648c0b5265805ef9bcc5e
출처 데이터셋
uspto-grants-2014_11
특허 번호
US08889704B2

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