1-(2-Fluorophenyl)piperazine → 1-(3-(1-tert-butyl-5-p-tolyl-1H-pyrazol-3-yl)propyl)-4-(2-fluorophenyl)piperazine

HRID 387011

반응식

HRID 387011 반응식
[C:1]([N:5]1[C:9]([C:10]2[CH:15]=[CH:14][C:13]([CH3:16])=[CH:12][CH:11]=2)=[CH:8][C:7]([CH2:17][CH2:18][CH:19]=O)=[N:6]1)([CH3:4])([CH3:3])[CH3:2].[F:21][C:22]1[CH:27]=[CH:26][CH:25]=[CH:24][C:23]=1[N:28]1[CH2:33][CH2:32][NH:31][CH2:30][CH2:29]1.CCN(C(C)C)C(C)C.[BH-](OC(C)=O)(OC(C)=O)OC(C)=O.[Na+]>>[C:1]([N:5]1[C:9]([C:10]2[CH:15]=[CH:14][C:13]([CH3:16])=[CH:12][CH:11]=2)=[CH:8][C:7]([CH2:17][CH2:18][CH2:19][N:31]2[CH2:30][CH2:29][N:28]([C:23]3[CH:24]=[CH:25][CH:26]=[CH:27][C:22]=3[F:21])[CH2:33][CH2:32]2)=[N:6]1)([CH3:4])([CH3:3])[CH3:2]

참가 물질

5

반응물 4

HCID 705291-(2-Fluorophenyl)piperazineHCID 81531DiisopropylethylamineHCID 5049666Sodium triacetoxyborohydrideHCID 866399173-(1-tert-butyl-5-p-tolyl-1H-pyrazol-3-yl)propanal

생성물 1

HCID 250652601-(3-(1-tert-butyl-5-p-tolyl-1H-pyrazol-3-yl)propyl)-4-(2-fluorophenyl)piperazine

실험 절차

79 mg (76%) of target compound was obtained by using a method same as in Example 1 by using 3-(1-tert-butyl-5-p-tolyl-1H-pyrazol-3-yl)propanal (60 mg, 0.222 mmol), 1-(2-fluorophenyl)piperazine (40 mg, 0.222 mmol), DIPEA (0.06 mL, 0.333 mmol) and NaBH(OAc)3 (141 mg, 0.666 mmol).

후처리

  1. custom79 mg (76%) of target compound was obtained

출처 및 근거

ORD 기록
ord-7ca6849f973c4062b04f45a7f9ae90ba
출처 데이터셋
uspto-grants-2013_02
특허 번호
US08372844B2

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