Ethanesulfonyl chloride → HCID 46195696, 화합물

HRID 881652노트

반응식

HRID 881652 반응식
[NH2:1][C:2]1[CH:3]=[C:4]([CH:26]=[CH:27][CH:28]=1)[CH2:5][O:6][C:7]1[CH:15]=[C:14]([F:16])[CH:13]=[C:12]([NH:17][C:18]2[CH:23]=[CH:22][C:21]([I:24])=[CH:20][C:19]=2[F:25])[C:8]=1[C:9]([NH2:11])=[O:10].[CH2:29]([S:31](Cl)(=[O:33])=[O:32])[CH3:30]>N1C=CC=CC=1.C(OCC)(=O)C>[CH2:29]([S:31]([NH:1][C:2]1[CH:3]=[C:4]([CH:26]=[CH:27][CH:28]=1)[CH2:5][O:6][C:7]1[CH:15]=[C:14]([F:16])[CH:13]=[C:12]([NH:17][C:18]2[CH:23]=[CH:22][C:21]([I:24])=[CH:20][C:19]=2[F:25])[C:8]=1[C:9]([NH2:11])=[O:10])(=[O:33])=[O:32])[CH3:30]

참가 물질

5

반응물 2

HCID 11667Ethanesulfonyl chlorideHCID 67304831HCID 67304831, 화합물2회

생성물 1

HCID 46195696HCID 46195696, 화합물수율 80%

시약·촉매·용매 2

HCID 1049Pyridine용매HCID 8857Ethyl Acetate용매

실험 절차

In analogy to GP 6b, 89 mg of 2-(3-Amino-benzyloxy)-4-fluoro-6-(2-fluoro-4-iodo-phenylamino)-benzamide (Intermediate 3.2; 0.18 mmol, 1 eq.) were dissolved in 0.75 mL pyridine, treated with 34 μL ethylsulfonyl chloride (0.36 mmol, 2 eq.). and stirred at rt for two days. the resulting mixture diluted with ethyl acetate, washed with water and the organic layers dried. Concentration in vacuo was followed by trituration to provide 84 mg of the desired compound (80% yield) with a melting point of 170° C.

후처리

  1. washwashed with water
  2. customthe organic layers dried
  3. concentrationConcentration in vacuo

출처 및 근거

ORD 기록
ord-df4243446bdc4679b84f2721236c09f1
출처 데이터셋
uspto-grants-2015_03
특허 번호
US08993630B2

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