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

HRID 38097

반응식

HRID 38097 반응식
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

참가 물질

4

반응물 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

생성물 1

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

시약·촉매·용매 1

HCID 887Methanol용매

반응 조건

온도
60 °C

실험 절차

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.

후처리

  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

출처 및 근거

ORD 기록
ord-3c989f9eec9e407984d3bf9a37863345
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08524707B2

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