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Methoxyacetic Acid → N-[5-(4-Methanesulfonyl-3-trifluoromethyl-phenyl)-4-methyl-thiazol-2-yl]-2-methoxy-acetamide

HRID 2247371
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HRID 2247371 반응식
[CH3:1][S:2]([C:5]1[CH:10]=[CH:9][C:8]([C:11]2[S:15][C:14]([NH2:16])=[N:13][C:12]=2[CH3:17])=[CH:7][C:6]=1[C:18]([F:21])([F:20])[F:19])(=[O:4])=[O:3].CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.[CH3:46][O:47][CH2:48][C:49](O)=[O:50].CCN(C(C)C)C(C)C>CN(C=O)C>[CH3:1][S:2]([C:5]1[CH:10]=[CH:9][C:8]([C:11]2[S:15][C:14]([NH:16][C:49](=[O:50])[CH2:48][O:47][CH3:46])=[N:13][C:12]=2[CH3:17])=[CH:7][C:6]=1[C:18]([F:21])([F:20])[F:19])(=[O:3])=[O:4]
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

6

반응물 4

HCID 12251Methoxyacetic AcidHCID 81531DiisopropylethylamineHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 574737494-Methyl-5-(4-(methylsulfonyl)-3-(trifluoromethyl)phenyl)thiazol-2-amine

생성물 1

HCID 86598425N-[5-(4-Methanesulfonyl-3-trifluoromethyl-phenyl)-4-methyl-thiazol-2-yl]-2-methoxy-acetamide

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

5-(4-Methanesulfonyl-3-trifluoromethyl-phenyl)-4-methyl-thiazol-2-ylamine (158a) (0.1 g, 0.3 mmol) is added to a solution of HATU (0.226 g, 0.6 mmol), methoxyacetic acid (0.046 ml, 0.6 mmol) and DIPEA (0.1 ml, 0.6 mmol) in DMF (7.5 ml). The reaction mixture was left to stir for 3 days at room temperature. The reaction mixture is filtered through basic alumina. The solvent is removed in vacuo and the product is purified by chromatography on silica eluting with ethyl acetate-hexane (3:1) to give the titled compound.

후처리

  1. waitThe reaction mixture was left
  2. filtrationThe reaction mixture is filtered through basic alumina
  3. customThe solvent is removed in vacuo
  4. customthe product is purified by chromatography on silica eluting with ethyl acetate-hexane (3:1)

출처 및 근거

ORD 기록
ord-1849a52abe934f05a3f8cc955155aa4c
출처 데이터셋
uspto-grants-2010_03
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07687637B2

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