2-Fluoro-5-methoxyphenylboronic acid → 5-Fluoro-6-(2-fluoro-5-methoxyphenyl)picolinic acid

HRID 1523495노트

반응식

HRID 1523495 반응식
Br[C:2]1[N:7]=[C:6]([C:8]([OH:10])=[O:9])[CH:5]=[CH:4][C:3]=1[F:11].[F:12][C:13]1[CH:18]=[CH:17][C:16]([O:19][CH3:20])=[CH:15][C:14]=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>[F:11][C:3]1[CH:4]=[CH:5][C:6]([C:8]([OH:10])=[O:9])=[N:7][C:2]=1[C:14]1[CH:15]=[C:16]([O:19][CH3:20])[CH:17]=[CH:18][C:13]=1[F:12]

참가 물질

4

반응물 2

HCID 41572112-Fluoro-5-methoxyphenylboronic acidHCID 534011946-Bromo-5-fluoropicolinic Acid

생성물 1

HCID 592266055-Fluoro-6-(2-fluoro-5-methoxyphenyl)picolinic acid수율 86%

시약·촉매·용매 1

HCID 178418807HCID 178418807, 화합물촉매

실험 절차

Method 1 was followed using 6-bromo-5-fluoropicolinic acid (1.0 equiv.) and 2-fluoro-5-methoxyphenylboronic acid (1.3 equiv.) and Pd(dppf)Cl2-DCM (0.15 equiv.) to give 5-fluoro-6-(2-fluoro-5-methoxyphenyl)picolinic acid in 86% yield. LC/MS=266.1 (M+H), Rt=0.79 min.

출처 및 근거

ORD 기록
ord-8e3910ea9a6e406eaee0c54c61867879
출처 데이터셋
uspto-grants-2015_07
특허 번호
US09079889B2

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