Hydrazine hydrate (1:1) → HCID 178473791, 화합물

HRID 2261685노트

반응식

HRID 2261685 반응식
[C:1]([N:4]1[CH2:9][CH2:8][CH:7]([C:10](OS(C2C=CC(C)=CC=2)(=O)=O)=[C:11]([C:14]2[S:15][C:16]3[CH:22]=[CH:21][CH:20]=[CH:19][C:17]=3[N:18]=2)[C:12]#[N:13])[CH2:6][CH2:5]1)(=O)[CH3:2].[OH2:34].[NH2:35][NH2:36]>CO>[NH2:13][C:12]1[NH:36][N:35]=[C:10]([CH:7]2[CH2:8][CH2:9][N:4]([C:1](=[O:34])[CH3:2])[CH2:5][CH2:6]2)[C:11]=1[C:14]1[S:15][C:16]2[CH:22]=[CH:21][CH:20]=[CH:19][C:17]=2[N:18]=1

참가 물질

4

반응물 2

HCID 24654Hydrazine hydrate (1:1)HCID 86608764HCID 86608764, 화합물

생성물 1

HCID 178473791HCID 178473791, 화합물수율 55%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

A mixture of the above prepared toluene-4-sulfonic acid 1-(1-acetylpiperidin-4-yl)-2-benzothiazol-2-yl-2-cyanovinyl ester (140 mg, 0.29 mmol) and hydrazine hydrate (25 mg, 0.5 mmol) in methanol was refluxed overnight. The solvent was evaporated and the residue was purified by flash column chromatography eluting with CH2Cl2:MeOH=20:1 to yield 54 mg (55%) of 1-[4-(5-amino-4-benzothiazol-2-yl-1H-pyrazol-3-yl)-piperidin-1-yl]-ethanone. MS (ES+): 342.1 (M+1, 100%).

후처리

  1. additionA mixture of the
  2. temperaturewas refluxed overnight
  3. customThe solvent was evaporated
  4. customthe residue was purified by flash column chromatography
  5. washeluting with CH2Cl2

출처 및 근거

ORD 기록
ord-6604d0053f4c4fef80d27dbe0c72ef31
출처 데이터셋
uspto-grants-2010_12
특허 번호
US07847101B2

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