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2-(2-Cyclopropylpyrimidin-5-yl)-2-(4,4-difluoropiperidin-1-yl)acetonitrile → 2-(2-Cyclopropylpyrimidin-5-yl)-2-(4,4-difluoropiperidin-1-yl)ethanamine

HRID 1482488
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인쇄 미리보기

반응식

HRID 1482488 반응식
[CH:1]1([C:4]2[N:9]=[CH:8][C:7]([CH:10]([N:13]3[CH2:18][CH2:17][C:16]([F:20])([F:19])[CH2:15][CH2:14]3)[C:11]#[N:12])=[CH:6][N:5]=2)[CH2:3][CH2:2]1>CO.[Ni]>[CH:1]1([C:4]2[N:9]=[CH:8][C:7]([CH:10]([N:13]3[CH2:18][CH2:17][C:16]([F:19])([F:20])[CH2:15][CH2:14]3)[CH2:11][NH2:12])=[CH:6][N:5]=2)[CH2:3][CH2:2]1
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

4

반응물 1

HCID 867160032-(2-Cyclopropylpyrimidin-5-yl)-2-(4,4-difluoropiperidin-1-yl)acetonitrile

생성물 1

HCID 867160022-(2-Cyclopropylpyrimidin-5-yl)-2-(4,4-difluoropiperidin-1-yl)ethanamine수율 8.7%

시약·촉매·용매 2

HCID 935Nickel촉매HCID 887Methanol용매

실험 절차

A mixture of 2-(2-cyclopropylpyrimidin-5-yl)-2-(4,4-difluoropiperidin-1-yl)acetonitrile (3.50 g, 126 mmol), Raney Ni (3.50 g) and NH3H2O (10 mL) in MeOH (150 mL) was degassed and purged with argon and H2, then stirred at room temperature under H2 (50 Psi) for 4 hours. The reaction mixture was filtered and concentrated in vacuum to give 2-(2-cyclopropylpyrimidin-5-yl)-2-(4,4-difluoropiperidin-1-yl)ethanamine as a yellow oil (3.10 g), which was used directly for next step without further purification.

후처리

  1. customwas degassed
  2. custompurged with argon and H2
  3. filtrationThe reaction mixture was filtered
  4. concentrationconcentrated in vacuum

출처 및 근거

ORD 기록
ord-f45cb956fe4446e6ad23fec72db925a5
출처 데이터셋
uspto-grants-2016_08
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09415055B2

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