1,2-Dichloroethane → 2-(4-Bromo-3,5-dimethyl-1H-pyrazol-1-yl)-1-(3-hydroxy-1-azetidinyl)ethanone

HRID 58066노트

반응식

HRID 58066 반응식
[Br:1][C:2]1[C:3]([CH3:12])=[N:4][N:5]([CH2:8][C:9]([OH:11])=O)[C:6]=1[CH3:7].[NH:13]1[CH2:16][CH:15]([OH:17])[CH2:14]1.C1C=CC2N(O)N=NC=2C=1.C(Cl)CCl.C(N(C(C)C)C(C)C)C>CN(C=O)C.CCOC(C)=O>[Br:1][C:2]1[C:3]([CH3:12])=[N:4][N:5]([CH2:8][C:9]([N:13]2[CH2:16][CH:15]([OH:17])[CH2:14]2)=[O:11])[C:6]=1[CH3:7]

참가 물질

8

반응물 5

HCID 111,2-DichloroethaneHCID 757711-HydroxybenzotriazoleHCID 81531DiisopropylethylamineHCID 8196162-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)acetic acidHCID 15142903-Hydroxyazetidine

생성물 1

HCID 897829192-(4-Bromo-3,5-dimethyl-1H-pyrazol-1-yl)-1-(3-hydroxy-1-azetidinyl)ethanone

시약·촉매·용매 2

HCID 6228Dimethylformamide용매HCID 8857Ethyl Acetate용매

실험 절차

To 2-(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)acetic acid (0.4 g, 1.716 mmol) in DMF (6 mL) were added azetidin-3-ol (0.151 g, 2.060 mmol), HOBt (0.301 g, 2.231 mmol), and EDC (0.461 g, 2.403 mmol), followed by N-ethyl-N-isopropylpropan-2-amine (1.495 mL, 8.58 mmol). The reaction mixture was stirred for 18 hours at room temperature. The crude reaction mixture was subsequently diluted with EtOAc, washed with brine, dried over Na2SO4, and concentrated to give the title compound, which was used without further purification.

후처리

  1. customThe crude reaction mixture
  2. washwashed with brine
  3. dry with materialdried over Na2SO4
  4. concentrationconcentrated

출처 및 근거

ORD 기록
ord-50b2cd0b08494a209af383aea6476a4e
출처 데이터셋
uspto-grants-2016_09
특허 번호
US09434743B2

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