Rapid construction of substituted 3-amino-1,5-benzothiazepin-4(5H)-one dipeptide scaffolds through an Ugi-4CR – Ullmann cross-coupling sequence
Author:
Affiliation:
1. Research Group of Organic Chemistry
2. Departments of Chemistry and Bioengineering Sciences
3. Vrije Universiteit Brussel
4. B-1000 Brussels
5. Belgium
6. Organic Synthesis
7. Department of Chemistry
8. University of Antwerp
9. 2020 Antwerp
Abstract
A 3-step methodology afforded the title compounds in moderate to good yields, with in silico and NMR conformational studies showing that the lowest energy conformers stabilize γ- and β-turn structures.
Funder
Fonds Wetenschappelijk Onderzoek
Agentschap Innoveren en Ondernemen
Publisher
Royal Society of Chemistry (RSC)
Subject
Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2018/OB/C7OB03094K
Reference25 articles.
1. 1,5-Benzothiazepine, a versatile pharmacophore: A review
2. Pyrrolo[1,5]benzoxa(thia)zepines as a New Class of Potent Apoptotic Agents. Biological Studies and Identification of an Intracellular Location of Their Drug Target
3. Synthesis of halogen-substituted 1,5-benzothiazepine derivatives and their vasodilating and hypotensive activities
4. (cis)-3-methyl-1,5-benzothiazepine-4-ones: potent analogs of the calcium channel blocker diltiazen
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