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Trifluoroacetic acid → 2-(5-(4-((1R,2S)-2-amino-3-fluoro-1-hydroxypropyl)phenyl)isoxazol-3-yl)acetonitrile

HRID 1500289
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인쇄 미리보기

반응식

HRID 1500289 반응식
[C:1]([CH2:3][C:4]1[CH:8]=[C:7]([C:9]2[CH:14]=[CH:13][C:12]([C@H:15]3[O:19]C(C)(C)[N:17](C(OC(C)(C)C)=O)[C@@H:16]3[CH2:29][F:30])=[CH:11][CH:10]=2)[O:6][N:5]=1)#[N:2].FC(F)(F)C(O)=O>C(Cl)Cl.C1(C)C=CC=CC=1>[NH2:17][C@H:16]([CH2:29][F:30])[C@@H:15]([C:12]1[CH:11]=[CH:10][C:9]([C:7]2[O:6][N:5]=[C:4]([CH2:3][C:1]#[N:2])[CH:8]=2)=[CH:14][CH:13]=1)[OH:19]
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참가 물질

5

반응물 2

HCID 6422Trifluoroacetic acidHCID 86713175(4S,5R)-tert-butyl 5-(4-(3-(cyanomethyl)isoxazol-5-yl)phenyl)-4-(fluoromethyl)-2,2-dimethyloxazolidine-3-carboxylate

생성물 1

HCID 867131762-(5-(4-((1R,2S)-2-amino-3-fluoro-1-hydroxypropyl)phenyl)isoxazol-3-yl)acetonitrile

시약·촉매·용매 2

HCID 1140Toluene용매HCID 6344Dichloromethane용매

실험 절차

The product of step 1 of Example 12 (50 mg, 0.12 mmol) in CH2Cl2 (2 mL) at 5° C. is treated with trifluoroacetic acid (0.5 mL), stirred 30 minutes at room temperature, diluted with toluene, and concentrated to give the title compound, which is carried on to the next step without purification m/z (Cl) 276 [M+H].

후처리

  1. concentrationconcentrated

출처 및 근거

ORD 기록
ord-c52ff02eea9b4601800a495da71c1689
출처 데이터셋
uspto-grants-2015_12
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09206126B2

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