Triethylamine → Tert-butyl 4-(2-(3-amino-6-(4-(isopropylsulfonyl)phenyl)pyrazine-2-carbonyl)hydrazinecarbonyl)benzylcarbamate

HRID 2204865

반응식

HRID 2204865 반응식
[NH2:1][C:2]1[C:3]([C:20]([NH:22][NH2:23])=[O:21])=[N:4][C:5]([C:8]2[CH:13]=[CH:12][C:11]([S:14]([CH:17]([CH3:19])[CH3:18])(=[O:16])=[O:15])=[CH:10][CH:9]=2)=[CH:6][N:7]=1.[C:24]([O:28][C:29]([NH:31][CH2:32][C:33]1[CH:41]=[CH:40][C:36]([C:37](O)=[O:38])=[CH:35][CH:34]=1)=[O:30])([CH3:27])([CH3:26])[CH3:25].C(N(CC)CC)C.CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.[B-](F)(F)(F)F>O>[NH2:1][C:2]1[C:3]([C:20]([NH:22][NH:23][C:37]([C:36]2[CH:35]=[CH:34][C:33]([CH2:32][NH:31][C:29](=[O:30])[O:28][C:24]([CH3:25])([CH3:26])[CH3:27])=[CH:41][CH:40]=2)=[O:38])=[O:21])=[N:4][C:5]([C:8]2[CH:9]=[CH:10][C:11]([S:14]([CH:17]([CH3:19])[CH3:18])(=[O:15])=[O:16])=[CH:12][CH:13]=2)=[CH:6][N:7]=1

참가 물질

6

반응물 4

HCID 8471TriethylamineHCID 8536054-(((tert-Butoxycarbonyl)amino)methyl)benzoic acidHCID 2733207O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborateHCID 594716323-Amino-6-(4-isopropylsulfonylphenyl)pyrazine-2-carbohydrazide

생성물 1

HCID 59471855Tert-butyl 4-(2-(3-amino-6-(4-(isopropylsulfonyl)phenyl)pyrazine-2-carbonyl)hydrazinecarbonyl)benzylcarbamate

시약·촉매·용매 1

HCID 962Water용매

실험 절차

3-amino-6-(4-isopropylsulfonylphenyl)pyrazine-2-carbohydrazide (100 mg, 0.2833 mmol) and 4-[(tert-butoxycarbonylamino)methyl]benzoic acid (71.19 mg, 0.2833 mmol) in dmf (1.000 mL) was treated with triethylamine (28.67 mg, 39.49 μL, 0.2833 mmol) followed by TBTU (109.2 mg, 0.3400 mmol) and the resulting solution stirred at room temperature overnight. The solution was poured dropwise onto rapidly stirred water (15 ml), stirred at room temperature for 1 h and then filtered to give the product as a pale yellow solid which was dried under high vacuum at 83° C. and then used directly in the next step without further purification (136 mg, 84%)

후처리

  1. stirringstirred at room temperature for 1 h
  2. filtrationfiltered

출처 및 근거

ORD 기록
ord-3bbb7f0356784063a21bbfc3e2d5270c
출처 데이터셋
uspto-grants-2016_06
특허 번호
US09365557B2

연결된 노트

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