Dimethylamine, hydrochloride → (5R)-2-[(2S)-2-(3,4-dichlorophenyl)-4-(dimethylamino)butyl]-1-oxo-1,2,3,4-tetrahydronaphtho[1,2-f][1,4]thiazepine-6-carbonitrile 5-oxide

反応式

[Cl:1][C:2]1[CH:3]=[C:4]([C@H:9]([CH2:30][CH:31]=O)[CH2:10][N:11]2[C:17](=[O:18])[C:16]3[C:19]4[C:24]([CH:25]=[C:26]([C:27]#[N:28])[C:15]=3[S@:14](=[O:29])[CH2:13][CH2:12]2)=[CH:23][CH:22]=[CH:21][CH:20]=4)[CH:5]=[CH:6][C:7]=1[Cl:8].Cl.[CH3:34][NH:35][CH3:36]>>[Cl:1][C:2]1[CH:3]=[C:4]([C@H:9]([CH2:30][CH2:31][N:35]([CH3:36])[CH3:34])[CH2:10][N:11]2[C:17](=[O:18])[C:16]3[C:19]4[C:24]([CH:25]=[C:26]([C:27]#[N:28])[C:15]=3[S@:14](=[O:29])[CH2:13][CH2:12]2)=[CH:23][CH:22]=[CH:21][CH:20]=4)[CH:5]=[CH:6][C:7]=1[Cl:8]

参加物

反応物 2

HCID 10473Dimethylamine, hydrochloride

HCID 86759590(5R)-2-[(2S)-2-(3,4-dichlorophenyl)4-oxobutyl]-1-oxo-1,2,3,4-tetrahydronaphtho[1,2-f][1,4]thiazepine-6-carbonitrile 5-oxide

生成物 1

HCID 69140743(5R)-2-[(2S)-2-(3,4-dichlorophenyl)-4-(dimethylamino)butyl]-1-oxo-1,2,3,4-tetrahydronaphtho[1,2-f][1,4]thiazepine-6-carbonitrile 5-oxide収率 92.6%

実験手順

By the method described in Example 79, Intermediate 78c (10 mg, 0.021 mmol) and dimethylamine hydrochloride (5 mg, 0.06 mmol) were converted to 10 mg of the title compound.

出典と根拠

ORDレコード: ord-64bd30a16b4b4d9a84e1b460ab1f47d2
出典データセット: uspto-grants-2005_01
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US06846814B2

反応ノート

読み込み中…