Synthese von 1,4-Diazepino[1,2-a]-indolen

Condensation of 1-(3-aminopropyl)-3-methyl-indole (1) with acetaldehyde or benzaldehyde by the Mannich reaction gave 1,4-diazepino[1,2-a]-indoles 2 and 3 respectively. The 1,4-diazepino[1,2-a]indole 9 was obtained by analogous acidcatalyzed cyclo-condensation of 1 with dimethyl-2-dimethoxyethylmalo...

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Main Authors: Hans Peter Härter, Othmar Schindler
Format: Article
Language:deu
Published: Swiss Chemical Society 1977-09-01
Series:CHIMIA
Online Access:https://www.chimia.ch/chimia/article/view/9390
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author Hans Peter Härter
Othmar Schindler
author_facet Hans Peter Härter
Othmar Schindler
author_sort Hans Peter Härter
collection DOAJ
description Condensation of 1-(3-aminopropyl)-3-methyl-indole (1) with acetaldehyde or benzaldehyde by the Mannich reaction gave 1,4-diazepino[1,2-a]-indoles 2 and 3 respectively. The 1,4-diazepino[1,2-a]indole 9 was obtained by analogous acidcatalyzed cyclo-condensation of 1 with dimethyl-2-dimethoxyethylmalonate (8), and 6,17, and 19 were obtained by intramolecular condensation of 5, 15, and 16 respectively. All these lactames could be readily reduced to the corresponding bases 7, 12, 18 and 20. Bischler-Napieralsky cyclization of 23 gave the diazepinoindole-butanoic acid derivative 25 as main product, together with the fully cyclized 24. Compound 25, after reduction, gave directly the diazepinoindole 26, which was also obtained by reduction of compound 24.
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spelling doaj-art-6d17bc2269354ce3a3ca192fa4d2ccea2025-08-20T02:29:54ZdeuSwiss Chemical SocietyCHIMIA0009-42932673-24241977-09-0131910.2533/chimia.1977.362Synthese von 1,4-Diazepino[1,2-a]-indolenHans Peter Härter0Othmar Schindler1Forschungsinstitut Wander (eine Sandoz Forschungsgruppe), Bern, SchweizForschungsinstitut Wander (eine Sandoz Forschungsgruppe), Bern, Schweiz Condensation of 1-(3-aminopropyl)-3-methyl-indole (1) with acetaldehyde or benzaldehyde by the Mannich reaction gave 1,4-diazepino[1,2-a]-indoles 2 and 3 respectively. The 1,4-diazepino[1,2-a]indole 9 was obtained by analogous acidcatalyzed cyclo-condensation of 1 with dimethyl-2-dimethoxyethylmalonate (8), and 6,17, and 19 were obtained by intramolecular condensation of 5, 15, and 16 respectively. All these lactames could be readily reduced to the corresponding bases 7, 12, 18 and 20. Bischler-Napieralsky cyclization of 23 gave the diazepinoindole-butanoic acid derivative 25 as main product, together with the fully cyclized 24. Compound 25, after reduction, gave directly the diazepinoindole 26, which was also obtained by reduction of compound 24. https://www.chimia.ch/chimia/article/view/9390
spellingShingle Hans Peter Härter
Othmar Schindler
Synthese von 1,4-Diazepino[1,2-a]-indolen
CHIMIA
title Synthese von 1,4-Diazepino[1,2-a]-indolen
title_full Synthese von 1,4-Diazepino[1,2-a]-indolen
title_fullStr Synthese von 1,4-Diazepino[1,2-a]-indolen
title_full_unstemmed Synthese von 1,4-Diazepino[1,2-a]-indolen
title_short Synthese von 1,4-Diazepino[1,2-a]-indolen
title_sort synthese von 1 4 diazepino 1 2 a indolen
url https://www.chimia.ch/chimia/article/view/9390
work_keys_str_mv AT hanspeterharter synthesevon14diazepino12aindolen
AT othmarschindler synthesevon14diazepino12aindolen