2,6-Difluorophenylboronic acid → Methyl 3-amino-6-(2,6-difluorophenyl)-5-fluoropicolinate

HRID 879139

반응식

HRID 879139 반응식
[NH2:1][C:2]1[C:3]([C:10]([O:12][CH3:13])=[O:11])=[N:4][C:5](Br)=[C:6]([F:8])[CH:7]=1.[F:14][C:15]1[CH:20]=[CH:19][CH:18]=[C:17]([F:21])[C:16]=1B(O)O>C1C=CC(P(C2C=CC=CC=2)[C-]2C=CC=C2)=CC=1.C1C=CC(P(C2C=CC=CC=2)[C-]2C=CC=C2)=CC=1.Cl[Pd]Cl.[Fe+2].C(Cl)Cl>[NH2:1][C:2]1[C:3]([C:10]([O:12][CH3:13])=[O:11])=[N:4][C:5]([C:16]2[C:15]([F:14])=[CH:20][CH:19]=[CH:18][C:17]=2[F:21])=[C:6]([F:8])[CH:7]=1

참가 물질

4

반응물 2

HCID 27343362,6-Difluorophenylboronic acidHCID 72698878Methyl 3-amino-6-bromo-5-fluoropicolinate

생성물 1

HCID 59226608Methyl 3-amino-6-(2,6-difluorophenyl)-5-fluoropicolinate수율 94%

시약·촉매·용매 1

HCID 178418807HCID 178418807, 화합물촉매

실험 절차

Method 1 was followed using methyl 3-amino-6-bromo-5-fluoropicolinate (1.0 equiv.) and 2,6-difluorophenylboronic acid (1.3 equiv.) and Pd(dppf)Cl2-DCM (0.05 equiv.) to give methyl 3-amino-6-(2,6-difluorophenyl)-5-fluoropicolinate in 94% yield. LCMS (m/z): 283.0 (MH+), Rt=0.76 min.

출처 및 근거

ORD 기록
ord-8cf6f76f4150418db871e091716e482f
출처 데이터셋
uspto-grants-2015_03
특허 번호
US08987457B2

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