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

HRID 993038Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 993038
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]

Komponenten

6

Edukt 4

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

Produkt 1

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

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 887MethanolLösungsmittel

Versuchsvorschrift

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.

Aufarbeitung

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

Quellen und Nachweise

ORD-Eintrag
ord-e4ca4b5ccfb248a393a17706a874de75
Quelldatensatz
uspto-grants-2002_10
Patentnummer
US06472386B1

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