Hexahydro-1,4-diazepine → N,N'-bis[[5-(3,4,5-Trimethoxyphenyl)-thiophen-2-yl]methyl]homopiperazine Dimaleate

HRID 993038ノート

反応式

HRID 993038 の反応式
O[CH2:2][C:3]1[S:4][C:5]([C:8]2[CH:13]=[C:12]([O:14][CH3:15])[C:11]([O:16][CH3:17])=[C:10]([O:18][CH3:19])[CH:9]=2)=[CH:6][CH:7]=1.Cl[CH2:21][C:22]1[S:23][C:24]([C:27]2[CH:32]=[C:31]([O:33][CH3:34])[C:30]([O:35][CH3:36])=[C:29]([O:37][CH3:38])[CH:28]=2)=[CH:25][CH:26]=1.[NH:39]1[CH2:45][CH2:44][CH2:43][NH:42][CH2:41][CH2:40]1.[C:46]([OH:53])(=[O:52])/[CH:47]=[CH:48]/[C:49]([OH:51])=[O:50]>CO>[C:46]([OH:53])(=[O:52])/[CH:47]=[CH:48]\[C:49]([OH:51])=[O:50].[C:46]([OH:53])(=[O:52])/[CH:47]=[CH:48]\[C:49]([OH:51])=[O:50].[CH3:19][O:18][C:10]1[CH:9]=[C:8]([C:5]2[S:4][C:3]([CH2:2][N:39]3[CH2:45][CH2:44][CH2:43][N:42]([CH2:21][C:22]4[S:23][C:24]([C:27]5[CH:32]=[C:31]([O:33][CH3:34])[C:30]([O:35][CH3:36])=[C:29]([O:37][CH3:38])[CH:28]=5)=[CH:25][CH:26]=4)[CH2:41][CH2:40]3)=[CH:7][CH:6]=2)[CH:13]=[C:12]([O:14][CH3:15])[C:11]=1[O:16][CH3:17]

参加物

6

反応物 4

HCID 68163Hexahydro-1,4-diazepineHCID 444972Fumaric AcidHCID 184084922-Hydroxymethyl-5-(3,4,5-trimethoxyphenyl)thiopheneHCID 184085302-Chloromethyl-5-(3,4,5-trimethoxyphenyl)thiophene

生成物 1

HCID 86758583N,N'-bis[[5-(3,4,5-Trimethoxyphenyl)-thiophen-2-yl]methyl]homopiperazine Dimaleate

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

実験手順

2-Hydroxymethyl-5-(3,4,5-trimethoxyphenyl)thiophene (230 mg) was treated in the same manner in Preparation Example 4 to synthesize 2-chloromethyl-5-(3,4,5-trimethoxyphenyl)thiophene. Since this product was unstable, it was immediately reacted with homopiperazine (41 mg) in the same manner in Example 1 without isolating it to obtain a product as a free base. This product was dissolved in methanol, and fumaric acid was added to the solution, thereby converting it into the title compound.

後処理

  1. customwithout isolating it
  2. customto obtain a product as a free base

出典と根拠

ORDレコード
ord-e4ca4b5ccfb248a393a17706a874de75
出典データセット
uspto-grants-2002_10
特許番号
US06472386B1

反応ノート

読み込み中…