Trans-4-amino-1-methyl-cyclohexanol → HCID 67500443, 화합물

HRID 1631331노트

반응식

HRID 1631331 반응식
[NH2:1][CH:2]1[CH2:7][CH2:6][C:5]([CH3:9])([OH:8])[CH2:4][CH2:3]1.[F:10][C:11]1[CH:16]=[CH:15][C:14]([F:17])=[CH:13][C:12]=1[C@H:18]1[CH2:22][CH2:21][CH2:20][N:19]1[C:23]1[CH:28]=[CH:27][N:26]2[N:29]=[CH:30][C:31]([C:32](O)=[O:33])=[C:25]2[N:24]=1>>[F:10][C:11]1[CH:16]=[CH:15][C:14]([F:17])=[CH:13][C:12]=1[C@H:18]1[CH2:22][CH2:21][CH2:20][N:19]1[C:23]1[CH:28]=[CH:27][N:26]2[N:29]=[CH:30][C:31]([C:32]([NH:1][CH:2]3[CH2:7][CH2:6][C:5]([OH:8])([CH3:9])[CH2:4][CH2:3]3)=[O:33])=[C:25]2[N:24]=1

참가 물질

3

반응물 2

HCID 18331273Trans-4-amino-1-methyl-cyclohexanolHCID 66847716HCID 66847716, 화합물

생성물 1

HCID 67500443HCID 67500443, 화합물수율 38%

실험 절차

The major isomer from Step A in Example 50 (45.1 mg, 0.197 mmol) was dissolved in DCM (1.0 mL) and 4N HCl in dioxane (492 μL, 1.97 mmol) was added. The reaction mixture was stirred at ambient temperature for 1 hour and was concentrated to afford 4-amino-1-methylcyclohexanol (major isomer). The 4-amino-1-methylcyclohexanol was reacted with (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxylic acid (Preparation C) according to the procedure outlined in Example 1 to provide the title product as a white solid (10.7 mg, 38% yield). MS (apci) m/z=456.1 (M+H).

출처 및 근거

ORD 기록
ord-c1f3779c1dbc4cfe971a786bd41b133d
출처 데이터셋
uspto-grants-2014_07
특허 번호
US08791123B2

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