5-(2,2,2-Trifluoroethoxy)pyridine-2-carboxylic acid → 5-(2,2,2-Trifluoro-ethoxy)-pyridine-2-carboxylic acid {3-[(4R,5R)-2-amino-4-methyl-5-(2,2,2-trifluoro-ethoxy)-5,6-dihydro-4H-[1,3]oxazin-4-yl]-4-fluoro-phenyl}-amide

HRID 405767

反応式

HRID 405767 の反応式
[NH2:1][C:2]1[CH:3]=[CH:4][C:5]([F:22])=[C:6]([C@:8]2([CH3:21])[C@@H:13]([O:14][CH2:15][C:16]([F:19])([F:18])[F:17])[CH2:12][O:11][C:10]([NH2:20])=[N:9]2)[CH:7]=1.[F:23][C:24]([F:37])([F:36])[CH2:25][O:26][C:27]1[CH:28]=[CH:29][C:30]([C:33](O)=[O:34])=[N:31][CH:32]=1>>[NH2:20][C:10]1[O:11][CH2:12][C@H:13]([O:14][CH2:15][C:16]([F:18])([F:19])[F:17])[C@:8]([C:6]2[CH:7]=[C:2]([NH:1][C:33]([C:30]3[CH:29]=[CH:28][C:27]([O:26][CH2:25][C:24]([F:37])([F:36])[F:23])=[CH:32][N:31]=3)=[O:34])[CH:3]=[CH:4][C:5]=2[F:22])([CH3:21])[N:9]=1

参加物

3

反応物 2

HCID 574758545-(2,2,2-Trifluoroethoxy)pyridine-2-carboxylic acidHCID 86672007(4R,5R)-4-(5-amino-2-fluoro-phenyl)-4-methyl-5-(2,2,2-trifluoro-ethoxy)-5,6-dihydro-4H-[1,3]oxazin-2-ylamine

生成物 1

HCID 665591005-(2,2,2-Trifluoro-ethoxy)-pyridine-2-carboxylic acid {3-[(4R,5R)-2-amino-4-methyl-5-(2,2,2-trifluoro-ethoxy)-5,6-dihydro-4H-[1,3]oxazin-4-yl]-4-fluoro-phenyl}-amide

実験手順

The condensation of (4R,5R)-4-(5-amino-2-fluoro-phenyl)-4-methyl-5-(2,2,2-trifluoro-ethoxy)-5,6-dihydro-4H-[1,3]oxazin-2-ylamine (A8.4) and 5-(2,2,2-trifluoro-ethoxy)-pyridine-2-carboxylic acid following procedure I yielded the title compound as a white solid. MS (ISP): m/z=525.2.

出典と根拠

ORDレコード
ord-4094627bfc68417f981033dec1a2ce06
出典データセット
uspto-grants-2014_06
特許番号
US08754075B2

関連ノート

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