5-bromo-N-(pyridin-3-yl)thiophene-2-sulfonamide → 5-[7-Difluoromethyl-5-(4-trifluoromethyl-phenyl)-pyrazolo[1,5-a]pyrimidin-3-ylethynyl]-thiophene-2-sulfonic acid pyridin-3-ylamide

HRID 558901ノート

反応式

HRID 558901 の反応式
[F:1][CH:2]([F:24])[C:3]1[N:8]2[N:9]=[CH:10][C:11]([C:12]#[CH:13])=[C:7]2[N:6]=[C:5]([C:14]2[CH:19]=[CH:18][C:17]([C:20]([F:23])([F:22])[F:21])=[CH:16][CH:15]=2)[CH:4]=1.[N:25]1[CH:30]=[CH:29][CH:28]=[C:27]([NH:31][S:32]([C:35]2[S:36][C:37](Br)=[CH:38][CH:39]=2)(=[O:34])=[O:33])[CH:26]=1>>[N:25]1[CH:30]=[CH:29][CH:28]=[C:27]([NH:31][S:32]([C:35]2[S:36][C:37]([C:13]#[C:12][C:11]3[CH:10]=[N:9][N:8]4[C:3]([CH:2]([F:1])[F:24])=[CH:4][C:5]([C:14]5[CH:19]=[CH:18][C:17]([C:20]([F:23])([F:22])[F:21])=[CH:16][CH:15]=5)=[N:6][C:7]=34)=[CH:38][CH:39]=2)(=[O:33])=[O:34])[CH:26]=1

参加物

3

反応物 2

HCID 9330735-bromo-N-(pyridin-3-yl)thiophene-2-sulfonamideHCID 866080343-Ethynyl-7-difluoromethyl-5-(4-trifluoromethyl-phenyl)-pyrazolo[1,5-a]pyrimidine

生成物 1

HCID 670012815-[7-Difluoromethyl-5-(4-trifluoromethyl-phenyl)-pyrazolo[1,5-a]pyrimidin-3-ylethynyl]-thiophene-2-sulfonic acid pyridin-3-ylamide

実験手順

The title compound was prepared from 7-difluoromethyl-3-ethynyl-5-(4-trifluoromethyl-phenyl)-pyrazolo[1,5-a]pyrimidine (example C.2) (169 mg, 0.5 mmol) and commercially available 5-bromo-thiophene-2-sulfonic acid pyridin-3-ylamide [CAS-No. 439934-18-6] (160 mg, 0.5 mmol) according to general procedure II. Obtained as a yellow solid (220 mg, 76%). MS (ISN) 574.1 [(M−H)−]; mp 226° C.

出典と根拠

ORDレコード
ord-2db632eff3534f2eaac91c82a4c83996
出典データセット
uspto-grants-2011_11
特許番号
US08063048B2

反応ノート

読み込み中…