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Synthesis 2013; 45(17): 2413-2416
DOI: 10.1055/s-0033-1339325
DOI: 10.1055/s-0033-1339325
paper
5,6,7,8-Tetrahydropyrido[4,3-c]pyridazine: A Lead-Oriented Scaffold with Two Diversity Points
Further Information
Publication History
Received: 17 April 2013
Accepted after revision: 07 June 2013
Publication Date:
10 July 2013 (online)
Abstract
An approach to the derivatives of 5,6,7,8-tetrahydropyrido[4,3-c]pyridazine, a lead-oriented scaffold with two diversity points, was developed. The method included five steps starting from the readily available 4-piperidone derivatives and allowed for the preparation of the target compounds in 32–35% overall yields. The key step of the sequence included one-pot solvent-free reaction of the corresponding 4-piperidone derivative, glyoxylic acid, and hydrazine.
Key words
nitrogen heterocycles - pyridazine - piperidine - nucleophilic substitution - lead-oriented synthesisSupporting Information
- for this article is available online at http://www.thieme-connect.com/ejournals/toc/synthesis.
- Supporting Information
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