Ammonia → 6-[3-(2,5-Difluoro-benzenesulfonylamino)-phenyl]-7-pyridin-4-yl-pyrazolo[5,1-b]thiazole-3-carboxylic acid amide

HRID 38098노트

반응식

HRID 38098 반응식
C(O[C:4]([C:6]1[N:7]2[N:13]=[C:12]([C:14]3[CH:19]=[CH:18][CH:17]=[C:16]([NH:20][S:21]([C:24]4[CH:29]=[C:28]([F:30])[CH:27]=[CH:26][C:25]=4[F:31])(=[O:23])=[O:22])[CH:15]=3)[C:11]([C:32]3[CH:37]=[CH:36][N:35]=[CH:34][CH:33]=3)=[C:8]2[S:9][CH:10]=1)=[O:5])C.[NH3:38]>CO>[F:31][C:25]1[CH:26]=[CH:27][C:28]([F:30])=[CH:29][C:24]=1[S:21]([NH:20][C:16]1[CH:15]=[C:14]([C:12]2[C:11]([C:32]3[CH:33]=[CH:34][N:35]=[CH:36][CH:37]=3)=[C:8]3[S:9][CH:10]=[C:6]([C:4]([NH2:38])=[O:5])[N:7]3[N:13]=2)[CH:19]=[CH:18][CH:17]=1)(=[O:23])=[O:22]

참가 물질

4

반응물 2

HCID 222AmmoniaHCID 674218916-[3-(2,5-Difluoro-benzenesulfonylamino)-phenyl]-7-pyridin-4-yl-pyrazolo[5,1-b]thiazole-3-carboxylic acid ethyl ester

생성물 1

HCID 467019716-[3-(2,5-Difluoro-benzenesulfonylamino)-phenyl]-7-pyridin-4-yl-pyrazolo[5,1-b]thiazole-3-carboxylic acid amide수율 93%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

6-[3-(2,5-Difluoro-benzenesulfonylamino)-phenyl]-7-pyridin-4-yl-pyrazolo[5,1-b]thiazole-3-carboxylic acid ethyl ester (30 mg, 0.055 mmol) was suspended a 7 N ammonia solution in methanol (1 mL) at 0° C. and stirred at this temperature for 18 hours. The mixture was evaporated to dryness and taken up with DCM and evaporated to dryness three times. The beige solid was dried under vacuum at room temperature to give 26 mg (93%) of 6-[3-(2,5-difluoro-benzenesulfonylamino)-phenyl]-7-pyridin-4-yl-pyrazolo[5,1-b]thiazole-3-carboxylic acid amide.

후처리

  1. customat 0° C.
  2. customThe mixture was evaporated to dryness
  3. customevaporated to dryness three times
  4. customThe beige solid was dried under vacuum at room temperature

출처 및 근거

ORD 기록
ord-9a871aeb26894528ad7380098e3fea80
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08524707B2

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