3-Chloro-5-cyanopyridine-2-carboxylic acid → 3-Chloro-5-cyano-pyridine-2-carboxylic acid [3-((4R,5S)-2-amino-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-4-fluoro-phenyl]-amide

HRID 517069

反応式

HRID 517069 の反応式
[NH2:1][C:2]1[CH:3]=[CH:4][C:5]([F:17])=[C:6]([C@:8]2([CH3:16])[C@H:13]([F:14])[CH2:12][O:11][C:10]([NH2:15])=[N:9]2)[CH:7]=1.[Cl:18][C:19]1[C:20]([C:27](O)=[O:28])=[N:21][CH:22]=[C:23]([C:25]#[N:26])[CH:24]=1>>[NH2:15][C:10]1[O:11][CH2:12][C@@H:13]([F:14])[C@:8]([C:6]2[CH:7]=[C:2]([NH:1][C:27]([C:20]3[C:19]([Cl:18])=[CH:24][C:23]([C:25]#[N:26])=[CH:22][N:21]=3)=[O:28])[CH:3]=[CH:4][C:5]=2[F:17])([CH3:16])[N:9]=1

参加物

3

反応物 2

HCID 508531763-Chloro-5-cyanopyridine-2-carboxylic acidHCID 86672005(4R,5S)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine

生成物 1

HCID 665588603-Chloro-5-cyano-pyridine-2-carboxylic acid [3-((4R,5S)-2-amino-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-4-yl)-4-fluoro-phenyl]-amide

実験手順

The condensation of (4R,5S)-4-(5-amino-2-fluoro-phenyl)-5-fluoro-4-methyl-5,6-dihydro-4H-[1,3]oxazin-2-ylamine (intermediate A8.1) and 3-chloro-5-cyano-pyridine-2-carboxylic acid following procedure I yielded the title compound as an off-white foam. MS (ISP): m/z=406.2 [M+H]+.

出典と根拠

ORDレコード
ord-f2e74413a26a4d8e9242f2b518498148
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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