Ammonia → 7-Pyridin-4-yl-6-{3-[3-(4-trifluoromethyl-phenyl)-ureido]-phenyl}-pyrazolo[5,1-b]thiazole-3-carboxylic acid amide

HRID 38097

反応式

HRID 38097 の反応式
C([O:3][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][C:21]([NH:23][C:24]4[CH:29]=[CH:28][C:27]([C:30]([F:33])([F:32])[F:31])=[CH:26][CH:25]=4)=[O:22])[CH:15]=3)[C:11]([C:34]3[CH:39]=[CH:38][N:37]=[CH:36][CH:35]=3)=[C:8]2[S:9][CH:10]=1)=O)C.[NH3:40]>CO>[N:37]1[CH:36]=[CH:35][C:34]([C:11]2[C:12]([C:14]3[CH:19]=[CH:18][CH:17]=[C:16]([NH:20][C:21]([NH:23][C:24]4[CH:29]=[CH:28][C:27]([C:30]([F:31])([F:33])[F:32])=[CH:26][CH:25]=4)=[O:22])[CH:15]=3)=[N:13][N:7]3[C:6]([C:4]([NH2:40])=[O:3])=[CH:10][S:9][C:8]=23)=[CH:39][CH:38]=1

参加物

4

反応物 2

HCID 222AmmoniaHCID 674240887-Pyridin-4-yl-6-{3-[3-(4-trifluoromethyl-phenyl)-ureido]-phenyl}-pyrazolo[5,1-b]thiazole-3-carboxylic acid ethyl ester

生成物 1

HCID 467019707-Pyridin-4-yl-6-{3-[3-(4-trifluoromethyl-phenyl)-ureido]-phenyl}-pyrazolo[5,1-b]thiazole-3-carboxylic acid amide収率 46%

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

反応条件

温度
60 °C

実験手順

7-Pyridin-4-yl-6-{3-[3-(4-trifluoromethyl-phenyl)-ureido]-phenyl}-pyrazolo[5,1-b]-thiazole-3-carboxylic acid ethyl ester (31 mg, 0.056 mmol) was suspended a 7 N ammonia solution in methanol (1.5 mL) in a screw cap Pyrex tube. The mixture was stirred at 60° C. for 32 hours and then allowed to cool slowly to room temperature during the night. The suspended solid was filtered, washed with DCM and dried at 50° C. under high vacuum to give 13 mg of 7-pyridin-4-yl-6-{3-[3-(4-trifluoromethyl-phenyl)-ureido]-phenyl}-pyrazolo[5,1-b]thiazole-3-carboxylic acid amide (46%) as off-white solid.

後処理

  1. customcap Pyrex tube
  2. temperatureto cool slowly to room temperature during the night
  3. filtrationThe suspended solid was filtered
  4. washwashed with DCM
  5. customdried at 50° C. under high vacuum

出典と根拠

ORDレコード
ord-3c989f9eec9e407984d3bf9a37863345
出典データセット
uspto-grants-2013_09
特許番号
US08524707B2

関連ノート

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