2,4-Difluoronitrobenzene → Tert-butyl 1-(5-fluoro-2-nitrophenyl)-piperidin-4-ylcarbamate

반응식

[F:1][C:2]1[CH:7]=[CH:6][C:5]([N+:8]([O-:10])=[O:9])=[C:4](F)[CH:3]=1.[C:12]([NH:19][CH:20]1[CH2:25][CH2:24][NH:23][CH2:22][CH2:21]1)([O:14][C:15]([CH3:18])([CH3:17])[CH3:16])=[O:13]>>[F:1][C:2]1[CH:7]=[CH:6][C:5]([N+:8]([O-:10])=[O:9])=[C:4]([N:23]2[CH2:22][CH2:21][CH:20]([NH:19][C:12](=[O:13])[O:14][C:15]([CH3:17])([CH3:16])[CH3:18])[CH2:25][CH2:24]2)[CH:3]=1

참가 물질

반응물 2

HCID 679672,4-Difluoronitrobenzene

HCID 7238334-(N-Boc-amino)piperidine

생성물 1

HCID 69044868Tert-butyl 1-(5-fluoro-2-nitrophenyl)-piperidin-4-ylcarbamate수율 93%

실험 절차

Method 1 was followed using 1 eq each of 1,3-difluoro-4-nitrobenzene, 4-(N-Boc-amino) piperidine, and TEA yielding tert-butyl 1-(5-fluoro-2-nitrophenyl)-piperidin-4-ylcarbamate (93%). LCMS (m/z): 340.1 (MH+); LC Rt=3.24 min.

출처 및 근거

ORD 기록: ord-b0546e3539b24065b65fdd9cab43f212
출처 데이터셋: uspto-grants-2014_09
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US08822497B2

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