Glyoxylic acid, monohydrate → 2-(5-Carbamoyl-2-fluorophenylamino)-2-(4-chloro-3-methoxyphenyl)acetic acid

HRID 1515518

反応式

HRID 1515518 の反応式
[C:1]([C:4]1[CH:5]=[C:6]([NH:10][CH:11](C2C=CC(OC)=C(OC)C=2)[C:12]([OH:14])=[O:13])[CH:7]=[CH:8][CH:9]=1)(=[O:3])[NH2:2].[Cl:25][C:26]1[CH:31]=[CH:30][C:29](B(O)O)=[CH:28][C:27]=1[O:35][CH3:36].NC1C=C(C=CC=1[F:47])C(N)=O.O.C(O)(=O)C=O>>[C:1]([C:4]1[CH:9]=[CH:8][C:7]([F:47])=[C:6]([NH:10][CH:11]([C:29]2[CH:30]=[CH:31][C:26]([Cl:25])=[C:27]([O:35][CH3:36])[CH:28]=2)[C:12]([OH:14])=[O:13])[CH:5]=1)(=[O:3])[NH2:2]

参加物

5

反応物 4

HCID 15620607Glyoxylic acid, monohydrateHCID 167821003-Amino-4-fluorobenzamideHCID 23005377(4-Chloro-3-methoxyphenyl)boronic acidHCID 598380342-(3-Carbamoylphenylamino)-2-(3,4-dimethoxyphenyl)acetic acid

生成物 1

HCID 594794212-(5-Carbamoyl-2-fluorophenylamino)-2-(4-chloro-3-methoxyphenyl)acetic acid収率 37%

実験手順

25B was prepared in a procedure similar to that of 1A using 25A, 19B and glyoxylic acid monohydrate. Yield: 37%. 1H NMR (400 MHz, Methanol-d4) δ ppm 3.88 (s, 3H) 5.21 (s, 1H) 7.03-7.12 (m, 3H) 7.13-7.19 (m, 1H) 7.25 (d, J=1.76 Hz, 1H) 7.33 (d, J=7.91 Hz, 1H), LCMS: 353 (M+1).

出典と根拠

ORDレコード
ord-50ffb40bb3e44f0594888b01a9be3601
出典データセット
uspto-grants-2012_07
特許番号
US08222453B2

関連ノート

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