Trifluoroacetic acid → N-[(1S,2S,5R)-7-methyl-3-aza-bicyclo[3.3.0]oct-2-ylmethyl]-2,2,2-trifluoro-acetamide

HRID 425800노트

반응식

HRID 425800 반응식
C(OC([N:8]1[CH2:15][C@H:14]2[C@H:10]([CH2:11][CH:12]([CH3:16])[CH2:13]2)[C@H:9]1[CH2:17][NH:18][C:19](=[O:24])[C:20]([F:23])([F:22])[F:21])=O)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[CH3:16][CH:12]1[CH2:11][C@H:10]2[C@H:14]([CH2:15][NH:8][C@@H:9]2[CH2:17][NH:18][C:19](=[O:24])[C:20]([F:23])([F:21])[F:22])[CH2:13]1

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 86643543(1S,2S,5R)-2-[(2,2,2-trifluoro-acetylamino)-methyl]-7-methyl-3-aza-bicyclo[3.3.0]-octane-3-carboxylic acid tert.-butyl ester

생성물 1

HCID 86643544N-[(1S,2S,5R)-7-methyl-3-aza-bicyclo[3.3.0]oct-2-ylmethyl]-2,2,2-trifluoro-acetamide

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

To a cold (0° C.) solution of (1S,2S,5R)-2-[(2,2,2-trifluoro-acetylamino)-methyl]-7-methyl-3-aza-bicyclo[3.3.0]-octane-3-carboxylic acid tert.-butyl ester (1.51 g) in DCM (13 mL) was slowly added TFA (3.31 mL, 10 eq). The reaction mixture was allowed to warm at RT and stirred overnight. Solvent and excess of TFA were removed in vacuo and the product was used for the next step without further purification.

후처리

  1. customSolvent and excess of TFA were removed in vacuo
  2. customthe product was used for the next step without further purification

출처 및 근거

ORD 기록
ord-09f31d8d967e47e9a5c4fb78cc1b43ed
출처 데이터셋
uspto-grants-2012_01
특허 번호
US08106215B2

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