3,4-Dimethoxyphenylboronic acid → 2-(5-Carbamoyl-2,4-difluorophenylamino)-2-(3,4-dimethoxyphenyl)acetic acid

HRID 1515516

반응식

HRID 1515516 반응식
[C:1]([C:4]1[CH:5]=[C:6]([NH:11][CH:12]([C:16]2[CH:21]=[CH:20][C:19]([O:22][CH3:23])=[C:18]([O:24][CH3:25])[CH:17]=2)[C:13]([OH:15])=[O:14])[CH:7]=[CH:8][C:9]=1[F:10])(=[O:3])[NH2:2].NC1C=C(C(F)=CC=1[F:36])C(N)=O.COC1C=C(B(O)O)C=CC=1OC.O.C(O)(=O)C=O>>[C:1]([C:4]1[C:9]([F:10])=[CH:8][C:7]([F:36])=[C:6]([NH:11][CH:12]([C:16]2[CH:21]=[CH:20][C:19]([O:22][CH3:23])=[C:18]([O:24][CH3:25])[CH:17]=2)[C:13]([OH:15])=[O:14])[CH:5]=1)(=[O:3])[NH2:2]

참가 물질

5

반응물 4

HCID 27347023,4-Dimethoxyphenylboronic acidHCID 15620607Glyoxylic acid, monohydrateHCID 256582395-Amino-2,4-difluorobenzamideHCID 594793922-(3-Carbamoyl-4-fluorophenylamino)-2-(3,4-dimethoxyphenyl)acetic acid

생성물 1

HCID 594794102-(5-Carbamoyl-2,4-difluorophenylamino)-2-(3,4-dimethoxyphenyl)acetic acid수율 80%

실험 절차

23A was prepared in a procedure similar to that of 13A using 3-amino-4,6-difluorobenzamide, 3,4-dimethoxyphenylboronic acid and glyoxylic acid monohydrate. Yield: 80%. 1H NMR (400 MHz, Methanol-d4) δ ppm 3.73-3.87 (m, 6H) 5.07 (s, 1H) 6.92 (t, J=7.69 Hz, 1H) 6.96-7.13 (m, 4H), LCMS: 367 (M+1).

출처 및 근거

ORD 기록
ord-aac2b33af5ec40a89882f778732b365d
출처 데이터셋
uspto-grants-2012_07
특허 번호
US08222453B2

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