Lithium Hexamethyldisilazide → N-(2,4-dimethoxybenzyl)-2,4,5-trifluoro-N-(2-fluoropyrimidin-4-yl)benzenesulfonamide

HRID 337748

反応式

HRID 337748 の反応式
[CH3:1][O:2][C:3]1[CH:17]=[C:16]([O:18][CH3:19])[CH:15]=[CH:14][C:4]=1[CH2:5][NH:6][C:7]1[CH:12]=[CH:11][N:10]=[C:9]([F:13])[N:8]=1.[Li+].C[Si]([N-][Si](C)(C)C)(C)C.[F:30][C:31]1[CH:36]=[C:35]([F:37])[C:34]([F:38])=[CH:33][C:32]=1[S:39](Cl)(=[O:41])=[O:40]>C1COCC1>[CH3:1][O:2][C:3]1[CH:17]=[C:16]([O:18][CH3:19])[CH:15]=[CH:14][C:4]=1[CH2:5][N:6]([C:7]1[CH:12]=[CH:11][N:10]=[C:9]([F:13])[N:8]=1)[S:39]([C:32]1[CH:33]=[C:34]([F:38])[C:35]([F:37])=[CH:36][C:31]=1[F:30])(=[O:41])=[O:40]

参加物

5

反応物 3

HCID 2733832Lithium HexamethyldisilazideHCID 27769792,4,5-Trifluorobenzenesulfonyl chlorideHCID 89963279N-(2,4-dimethoxybenzyl)-2-fluoropyrimidin-4-amine

生成物 1

HCID 89962306N-(2,4-dimethoxybenzyl)-2,4,5-trifluoro-N-(2-fluoropyrimidin-4-yl)benzenesulfonamide収率 63.3%

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

実験手順

The reaction and aftertreatment were conducted in the same manner as in Example 15a by using the N-(2,4-dimethoxybenzyl)-2-fluoropyrimidin-4-amine (0.20 g, 0.76 mmol) prepared in Example 24a, LiHMDS (1.0 M in THF, 0.91 mL, 0.91 mmol), 2,4,5-trifluorobenzenesulfonyl chloride (0.19 g, 0.84 mmol) and THF (3.0 mL), to yield the title compound (0.22 g, 63%) as a colorless solid.

後処理

  1. customThe reaction and aftertreatment

出典と根拠

ORDレコード
ord-c080981990e64642bd29a8453a34e9a2
出典データセット
uspto-grants-2014_11
特許番号
US08889741B2

関連ノート

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