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Triethylamine → N-[5-(3,5-difluoro-benzenesulfonyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide

HRID 1640992
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HRID 1640992 반응식
[F:1][C:2]1[CH:3]=[C:4]([S:9]([C:12]2[CH:13]=[C:14]3[C:18](=[CH:19][CH:20]=2)[NH:17][N:16]=[C:15]3[NH:21][C:22](=[O:49])[C:23]2[CH:28]=[CH:27][C:26]([N:29]3[CH2:34][CH2:33][N:32]([CH3:35])[CH2:31][CH2:30]3)=[CH:25][C:24]=2[N:36]([CH:43]2[CH2:48][CH2:47][O:46][CH2:45][CH2:44]2)C(=O)C(F)(F)F)(=[O:11])=[O:10])[CH:5]=[C:6]([F:8])[CH:7]=1.C(N(CC)CC)C>CO>[F:1][C:2]1[CH:3]=[C:4]([S:9]([C:12]2[CH:13]=[C:14]3[C:18](=[CH:19][CH:20]=2)[NH:17][N:16]=[C:15]3[NH:21][C:22](=[O:49])[C:23]2[CH:28]=[CH:27][C:26]([N:29]3[CH2:30][CH2:31][N:32]([CH3:35])[CH2:33][CH2:34]3)=[CH:25][C:24]=2[NH:36][CH:43]2[CH2:48][CH2:47][O:46][CH2:45][CH2:44]2)(=[O:10])=[O:11])[CH:5]=[C:6]([F:8])[CH:7]=1
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참가 물질

4

반응물 2

HCID 8471TriethylamineHCID 86643844N-[5-(3,5-difluoro-benzenesulfonyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-[(tetrahydro-pyran-4-yl)-(2,2,2-trifluoro-acetyl)-amino]-benzamide

생성물 1

HCID 59437080N-[5-(3,5-difluoro-benzenesulfonyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide수율 81.9%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

A mixture of N-[5-(3,5-difluoro-benzenesulfonyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-[(tetrahydro-pyran-4-yl)-(2,2,2-trifluoro-acetyl)-amino]-benzamide (1.41 g, 2.0 mmol), triethylamine (5.6 mL) and methanol (30 mL) was stirred at room temperature overnight. The solvents were removed under reduced pressure and the residue treated with methanol (10 mL), stirred at 45° C. for 30 minutes, filtered and dried in oven affording 1.0 g of the title compound as a white solid (81% yield).

후처리

  1. customThe solvents were removed under reduced pressure
  2. additionthe residue treated with methanol (10 mL)
  3. stirringstirred at 45° C. for 30 minutes
  4. filtrationfiltered
  5. customdried in oven

출처 및 근거

ORD 기록
ord-c03d247b12c5430ca7131ce17bfd9f46
출처 데이터셋
uspto-grants-2012_02
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08114865B2

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