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Trifluoroacetic acid → N-[(1R,2R)-1-amino-2,3-dihydro-1H-inden-2-yl]-2-chloro-6H-thieno[2,3-b]pyrrole-5-carboxamide

HRID 1244733
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HRID 1244733 반응식
C(OC(=O)[NH:7][C@@H:8]1[C:16]2[C:11](=[CH:12][CH:13]=[CH:14][CH:15]=2)[CH2:10][C@H:9]1[NH:17][C:18]([C:20]1[NH:24][C:23]2[S:25][C:26]([Cl:28])=[CH:27][C:22]=2[CH:21]=1)=[O:19])(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[NH2:7][C@@H:8]1[C:16]2[C:11](=[CH:12][CH:13]=[CH:14][CH:15]=2)[CH2:10][C@H:9]1[NH:17][C:18]([C:20]1[NH:24][C:23]2[S:25][C:26]([Cl:28])=[CH:27][C:22]=2[CH:21]=1)=[O:19]
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참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 58717460tert-Butyl((1R,2R)-2-{[(2-Chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino}-2,3-dihydro-1H-inden-1-yl)carbamate

생성물 1

HCID 58717470N-[(1R,2R)-1-amino-2,3-dihydro-1H-inden-2-yl]-2-chloro-6H-thieno[2,3-b]pyrrole-5-carboxamide수율 134.1%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

tert-Butyl((1R,2R)-2-{[(2-Chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino}-2,3-dihydro-1H-inden-1-yl)carbamate (Method 22, 10.6 g, 24.5 mmol) was suspended in DCM (200 mL), TFA (20 mL) added and the reaction stirred at ambient temperature for 20 hours. The volatiles were removed by evaporation under reduced pressure and the residue triturated with DCM (50 mL) then filtered and dried to give the title compound (10.9 g, 100%) as the trifluoroacetic acid salt.

후처리

  1. customThe volatiles were removed by evaporation under reduced pressure
  2. customthe residue triturated with DCM (50 mL)
  3. filtrationthen filtered
  4. customdried

출처 및 근거

ORD 기록
ord-eb50ff18a4cc4f04a8d66617580ae58f
출처 데이터셋
uspto-grants-2006_10
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07122567B2

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