Trifluoroacetic acid → (6S,7S)-5-methyl-6-[({4-[(2-methylquinolin-4-yl)methoxy]phenyl}amino)carbonyl]-5-azaspiro[2.5]octane-7-carboxylic acid

HRID 1664615노트

반응식

HRID 1664615 반응식
C(O)(C(F)(F)F)=O.[CH3:8][N:9]1[C@H:16]([C:17]([NH:19][C:20]2[CH:25]=[CH:24][C:23]([O:26][CH2:27][C:28]3[C:37]4[C:32](=[CH:33][CH:34]=[CH:35][CH:36]=4)[N:31]=[C:30]([CH3:38])[CH:29]=3)=[CH:22][CH:21]=2)=[O:18])[C@@H:15]([C:39]([O:41]C(C)(C)C)=[O:40])[CH2:14][C:11]2([CH2:13][CH2:12]2)[CH2:10]1>C(Cl)Cl>[CH3:8][N:9]1[C@H:16]([C:17]([NH:19][C:20]2[CH:21]=[CH:22][C:23]([O:26][CH2:27][C:28]3[C:37]4[C:32](=[CH:33][CH:34]=[CH:35][CH:36]=4)[N:31]=[C:30]([CH3:38])[CH:29]=3)=[CH:24][CH:25]=2)=[O:18])[C@@H:15]([C:39]([OH:41])=[O:40])[CH2:14][C:11]2([CH2:13][CH2:12]2)[CH2:10]1

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 67007475tert-butyl (6S,7S)-5-methyl-6-[({4-[(2-methylquinolin-4-yl)methoxy]phenyl}amino)carbonyl]-5-azaspiro[2.5]octane-7-carboxylate

생성물 1

HCID 67006214(6S,7S)-5-methyl-6-[({4-[(2-methylquinolin-4-yl)methoxy]phenyl}amino)carbonyl]-5-azaspiro[2.5]octane-7-carboxylic acid수율 149.6%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

TFA (1.0 mL) was added to a solution of tert-butyl (6S,7S)-5-methyl-6-[({4-[(2-methylquinolin-4-yl)methoxy]phenyl}amino)carbonyl]-5-azaspiro[2.5]octane-7-carboxylate (105.0 mg) in CH2Cl2 (1.0 mL) and the mixture was stirred at room temperature for 5 h. The solvent was removed to provide (6S,7S)-5-methyl-6-[({4-[(2-methylquinolin-4-yl)methoxy]phenyl}amino)carbonyl]-5-azaspiro[2.5]octane-7-carboxylic acid (140 mg) as an TFA salt. ESI (M+H)+ 460.3.

후처리

  1. customThe solvent was removed

출처 및 근거

ORD 기록
ord-24df2a77d458418484157a3b17d73840
출처 데이터셋
uspto-grants-2011_10
특허 번호
US08039471B2

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