Trifluoroacetic acid → (S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-{[5-(2-guanidinocarbonyl-cyclopropyl)-thiophene-2-carbonyl]-amino}-propionic acid

HRID 431512노트

반응식

HRID 431512 반응식
C([O:5][C:6](=[O:44])[C@@H:7]([NH:29][C:30]([O:32][CH2:33][C:34]12[CH2:43][CH:38]3[CH2:39][CH:40]([CH2:42][CH:36]([CH2:37]3)[CH2:35]1)[CH2:41]2)=[O:31])[CH2:8][NH:9][C:10]([C:12]1[S:13][C:14]([CH:17]2[CH2:19][CH:18]2[C:20](=[O:28])[NH:21][C:22]2[NH:23][CH2:24][CH2:25][CH2:26][N:27]=2)=[CH:15][CH:16]=1)=[O:11])(C)(C)C.FC(F)(F)C(O)=O>ClCCl>[C:34]12([CH2:33][O:32][C:30]([NH:29][C@@H:7]([CH2:8][NH:9][C:10]([C:12]3[S:13][C:14]([CH:17]4[CH2:19][CH:18]4[C:20](=[O:28])[NH:21][C:22]4[NH:23][CH2:24][CH2:25][CH2:26][N:27]=4)=[CH:15][CH:16]=3)=[O:11])[C:6]([OH:44])=[O:5])=[O:31])[CH2:43][CH:38]3[CH2:39][CH:40]([CH2:42][CH:36]([CH2:37]3)[CH2:35]1)[CH2:41]2

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 69637307(2s)-2-(1-Adamantylmethoxycarbonylamino)-3-((5-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)-cyclopropyl)-thiophene-2-carbonyl)-amino)-propionic acid tert-butyl ester

생성물 1

HCID 15859414(S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-{[5-(2-guanidinocarbonyl-cyclopropyl)-thiophene-2-carbonyl]-amino}-propionic acid

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

48 mg of the product obtained in step c) were dissolved in 2 ml of dichloromethane and stirred for 3 hours with 1 ml of trifluoroacetic acid under an inert gas atmosphere at room temperature. The solvents were removed in vacuo, the residue was dissolved in acetic acid and the solution was again evaporated to dryness. This procedure was repeated once. The resinous residue was triturated with diethyl ether. After filtration 30 mg of the title compound were obtained as a colourless amorphous powder.

후처리

  1. customThe solvents were removed in vacuo
  2. dissolutionthe residue was dissolved in acetic acid
  3. customthe solution was again evaporated to dryness
  4. customThe resinous residue was triturated with diethyl ether
  5. filtrationAfter filtration 30 mg of the title compound
  6. customwere obtained as a colourless amorphous powder

출처 및 근거

ORD 기록
ord-f278c3acc218494c857f105e01a0a97c
출처 데이터셋
uspto-grants-2003_12
특허 번호
US06660728B2

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