O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate → N-[6-chloro-4-(5-fluoro-2,3-dihydro-indole-1-carbonyl)-pyridin-2-yl]-methanesulphonamide

HRID 74585

反応式

HRID 74585 の反応式
[Cl:1][C:2]1[CH:3]=[C:4]([CH:8]=[C:9]([NH:11][S:12]([CH3:15])(=[O:14])=[O:13])[N:10]=1)[C:5]([OH:7])=O.[F:16][C:17]1[CH:18]=[C:19]2[C:23](=[CH:24][CH:25]=1)[NH:22][CH2:21][CH2:20]2.CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.[B-](F)(F)(F)F>CN(C=O)C>[Cl:1][C:2]1[N:10]=[C:9]([NH:11][S:12]([CH3:15])(=[O:14])=[O:13])[CH:8]=[C:4]([C:5]([N:22]2[C:23]3[C:19](=[CH:18][C:17]([F:16])=[CH:25][CH:24]=3)[CH2:20][CH2:21]2)=[O:7])[CH:3]=1

参加物

5

反応物 3

HCID 2733207O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborateHCID 27744635-FluoroindolineHCID 866564982-Chloro-6-methanesulphonylamino-isonicotinic acid

生成物 1

HCID 58386691N-[6-chloro-4-(5-fluoro-2,3-dihydro-indole-1-carbonyl)-pyridin-2-yl]-methanesulphonamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

0.28 g (1.1 mmol) 2-chloro-6-methanesulphonylamino-isonicotinic acid, 0.16 g (1.1 mmol) 5-fluoro-2,3-dihydro-1H-indole, 0.31 mL (2.2 mmol) TEA in 4.0 mL DMF were mixed with 0.39 g (1.2 mmol) TBTU and stirred for 2 h at RT. The reaction mixture was purified by HPLC. The product fractions were combined and evaporated down.

後処理

  1. customThe reaction mixture was purified by HPLC
  2. customevaporated down

出典と根拠

ORDレコード
ord-e79c9f683b0c4d6392fa55d1e6acb89d
出典データセット
uspto-grants-2014_09
特許番号
US08829006B2

関連ノート

読み込み中…