Pivaloyl chloride → 2,6-Difluoro-3-(tert-butylcarbonylamino-methyl)-benzoic acid

반응식

[NH2:1][CH2:2][C:3]1[C:4]([F:13])=[C:5]([C:9]([F:12])=[CH:10][CH:11]=1)[C:6]([OH:8])=[O:7].[C:14](Cl)([C:16]([CH3:19])([CH3:18])[CH3:17])=[O:15].FC(F)(F)C(=N[Si](C)(C)C)O[Si](C)(C)C.CSC1C2C(=CC(Br)=CC=2Br)NC=1SC>C1COCC1>[F:13][C:4]1[C:3]([CH2:2][NH:1][C:14]([C:16]([CH3:19])([CH3:18])[CH3:17])=[O:15])=[CH:11][CH:10]=[C:9]([F:12])[C:5]=1[C:6]([OH:8])=[O:7]

참가 물질

실험 절차

Prepared analogously to 44b with 3-aminomethyl-2,6-difluorobenzoic acid, Piv-Cl, BSTFA and TEA in THF. Yield: 1.2 g (77%); MS: [m+H]+=272; HPLC: Rt=1.38 min (Method MC-6)

출처 및 근거

ORD 기록: ord-f7cbc469eec047fc85d558065fc6414c
출처 데이터셋: uspto-grants-2015_02
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US08951999B2

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참가 물질

반응물 4

HCID 62493Pivaloyl chloride

HCID 94358Bis(trimethylsilyl)trifluoroacetamide

HCID 141858534,6-Dibromo-2,3-bis(methylsulfanyl)-1H-indole

HCID 584834803-(Aminomethyl)-2,6-difluorobenzoic acid

생성물 1

HCID 584833392,6-Difluoro-3-(tert-butylcarbonylamino-methyl)-benzoic acid

시약·촉매·용매 1

HCID 8028Tetrahydrofuran용매

실험 절차

Prepared analogously to 44b with 3-aminomethyl-2,6-difluorobenzoic acid, Piv-Cl, BSTFA and TEA in THF. Yield: 1.2 g (77%); MS: [m+H]+=272; HPLC: Rt=1.38 min (Method MC-6)

출처 및 근거

ORD 기록: ord-f7cbc469eec047fc85d558065fc6414c
출처 데이터셋: uspto-grants-2015_02
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US08951999B2

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