Water → (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)-3-cyclopropylpropanamide

HRID 2200406노트

반응식

HRID 2200406 반응식
[Cl:1][C:2]1[C:3]([C:9]#[N:10])=[N:4][CH:5]=[C:6](Cl)[N:7]=1.Cl.[NH2:12][C@H:13]([CH2:17][CH:18]1[CH2:20][CH2:19]1)[C:14]([NH2:16])=[O:15].CCN(C(C)C)C(C)C.O>CN1C(=O)CCC1.CCOC(C)=O>[Cl:1][C:2]1[N:7]=[C:6]([NH:12][C@H:13]([CH2:17][CH:18]2[CH2:20][CH2:19]2)[C:14]([NH2:16])=[O:15])[CH:5]=[N:4][C:3]=1[C:9]#[N:10]

참가 물질

7

반응물 4

HCID 962WaterHCID 81531DiisopropylethylamineHCID 529877443,5-Dichloropyrazine-2-carbonitrileHCID 67509203(R)-2-amino-3-cyclopropylpropanamide hydrochloride

생성물 1

HCID 86685539(R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)-3-cyclopropylpropanamide수율 99.5%

시약·촉매·용매 2

HCID 8857Ethyl Acetate용매HCID 13387N-methyl-2-pyrrolidone용매

실험 절차

A solution of 3,5-dichloropyrazine-2-carbonitrile (158 mg, 0.908 mmol), (R)-2-amino-3-cyclopropylpropanamide hydrochloride (150 mg, 0.911 mmol) and DIEA (0.400 mL, 2.30 mmol) in NMP (5 mL) was stirred at room temperature for 20 h. Water and EtOAc were added. Organic phase was separated, dried over Na2SO4, concentrated in vacuo to give (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)-3-cyclopropylpropanamide (240 mg).

후처리

  1. customOrganic phase was separated
  2. dry with materialdried over Na2SO4
  3. concentrationconcentrated in vacuo

출처 및 근거

ORD 기록
ord-6b0090a5ad514bf0809d67de74160f5e
출처 데이터셋
uspto-grants-2016_06
특허 번호
US09359308B2

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