Trifluoroacetic acid → [5-Cyano-2-cyclopropyl-4-(trifluoromethyl)-1H-indol-1-yl]acetic acid

HRID 913757

반응식

HRID 913757 반응식
[C:1]([C:3]1[C:4]([C:23]([F:26])([F:25])[F:24])=[C:5]2[C:9](=[CH:10][CH:11]=1)[N:8]([CH2:12][C:13]([O:15]C(C)(C)C)=[O:14])[C:7]([CH:20]1[CH2:22][CH2:21]1)=[CH:6]2)#[N:2].C(O)(C(F)(F)F)=O>C(Cl)Cl>[C:1]([C:3]1[C:4]([C:23]([F:26])([F:25])[F:24])=[C:5]2[C:9](=[CH:10][CH:11]=1)[N:8]([CH2:12][C:13]([OH:15])=[O:14])[C:7]([CH:20]1[CH2:22][CH2:21]1)=[CH:6]2)#[N:2]

참가 물질

4

반응물 2

HCID 6422Trifluoroacetic acidHCID 711086661,1-Dimethylethyl [5-cyano-2-cyclopropyl-4-(trifluoromethyl)-1H-indol-1-yl]acetate

생성물 1

HCID 67406028[5-Cyano-2-cyclopropyl-4-(trifluoromethyl)-1H-indol-1-yl]acetic acid수율 85.2%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

To a suspension of 1,1-dimethylethyl [5-cyano-2-cyclopropyl-4-(trifluoromethyl)-1H-indol-1-yl]acetate (Example 362A) (1.23 g, 4 mmol) in dry CH2Cl2 (10 mL) was added TFA (3.1 mL, 40 mmol) at rt. The mixture was stirred at rt overnight. Solvent and excess TFA were removed in vacuo. The residue was tritrated with Et2O-hexanes to afford the title compound (1.05 g, 85%): MS (ES) m/z 309 (M+1).

후처리

  1. customSolvent and excess TFA were removed in vacuo

출처 및 근거

ORD 기록
ord-2b92ca34957447e3a231633bfd58f4ce
출처 데이터셋
uspto-grants-2011_09
특허 번호
US08026262B2

연결된 노트

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