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

HRID 38098ノート

反応式

HRID 38098 の反応式
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]

参加物

4

反応物 2

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

生成物 1

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

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

実験手順

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.

後処理

  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

出典と根拠

ORDレコード
ord-9a871aeb26894528ad7380098e3fea80
出典データセット
uspto-grants-2013_09
特許番号
US08524707B2

反応ノート

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