3,5-Dichloro-2-pyridinecarboxylic acid → 3,5-Dichloro-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 517086

反応式

HRID 517086 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.[Cl:23][C:24]1[C:25]([C:31](O)=[O:32])=[N:26][CH:27]=[C:28]([Cl:30])[CH:29]=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:31]([C:25]3[C:24]([Cl:23])=[CH:29][C:28]([Cl:30])=[CH:27][N:26]=3)=[O:32])[CH:3]=[CH:4][C:5]=2[F:22])([CH3:21])[N:9]=1

参加物

3

反応物 2

HCID 2199893,5-Dichloro-2-pyridinecarboxylic 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 665579083,5-Dichloro-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 3,5-dichloro-pyridine-2-carboxylic acid following procedure I yielded the title compound as a white solid. MS (ISP): m/z=495.1 [M+H]+ and 497.2 [M+2+H]+.

出典と根拠

ORDレコード
ord-828032b0b2f8462ea1090ba38ea71343
出典データセット
uspto-grants-2015_08
特許番号
US09115098B2

関連ノート

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