(1S,4S)-2-Methyl-2,5-diazabicyclo[2.2.1]heptane → 4-((1S,4S)-2-Methyl-2,5-diazabicyclo[2.2.1]heptyl)-1-(2-methylbenzenesulfonyl)-1H-indole

HRID 8334

反応式

HRID 8334 の反応式
Br[C:2]1[CH:10]=[CH:9][CH:8]=[C:7]2[C:3]=1[CH:4]=[CH:5][N:6]2[S:11]([C:14]1[CH:19]=[CH:18][CH:17]=[CH:16][C:15]=1[CH3:20])(=[O:13])=[O:12].[CH3:21][N:22]1[CH2:27][C@@H:26]2[CH2:28][C@H:23]1[CH2:24][NH:25]2>>[CH3:21][N:22]1[CH2:27][C@@H:26]2[CH2:28][C@:23]1([C:2]1[CH:10]=[CH:9][CH:8]=[C:7]3[C:3]=1[CH:4]=[CH:5][N:6]3[S:11]([C:14]1[CH:19]=[CH:18][CH:17]=[CH:16][C:15]=1[CH3:20])(=[O:13])=[O:12])[CH2:24][NH:25]2

参加物

3

反応物 2

HCID 11029795(1S,4S)-2-Methyl-2,5-diazabicyclo[2.2.1]heptaneHCID 220153344-Bromo-1-(2-methyl-benzenesulfonyl)-1H-indole

生成物 1

HCID 689968374-((1S,4S)-2-Methyl-2,5-diazabicyclo[2.2.1]heptyl)-1-(2-methylbenzenesulfonyl)-1H-indole収率 19%

実験手順

The compound was prepared from 4-bromo-1-(2-methyl-benzenesulfonyl)-1H-indole and (1S,4S)-2-methyl-2,5-diazabicyclo[2.2.1]heptane according to Method 1 to give 25 mg (19%) of a white solid: 1H NMR (CD3OD) δ 7.91–6.44 (m, 9H), 4.67–4.63 (m, 1H), 4.35–4.33 (m, 1H), 4.09–4.07 (m, 1H), 3.99–3.95 (m, 1H), 3.72–3.70 (m, 1H), 3.21–3.17 (m, 1H), 2.95 (s, 3H), 2.33–2.31 (m, 2H); MS (ESI) 382.1 (M+H)+; Purity (HPLC) >95%.

出典と根拠

ORDレコード
ord-70012c0a48024771b36f75aabd29de67
出典データセット
uspto-grants-2006_08
特許番号
US07087750B2

関連ノート

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