Chiral azole derivatives. Part 5: Synthesis of enantiomerically pure 1-[alpha-(benzofuran-2-yl)arylmethyl]-1H-1,2,4-triazoles, antifungal and antiaromatase agents

Authors
Messina, F Botta, M Corelli, F Paladino, A
Citation
F. Messina et al., Chiral azole derivatives. Part 5: Synthesis of enantiomerically pure 1-[alpha-(benzofuran-2-yl)arylmethyl]-1H-1,2,4-triazoles, antifungal and antiaromatase agents, TETRAHEDR-A, 11(24), 2000, pp. 4895-4901
Citations number
12
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON-ASYMMETRY
ISSN journal
09574166 → ACNP
Volume
11
Issue
24
Year of publication
2000
Pages
4895 - 4901
Database
ISI
SICI code
0957-4166(200012)11:24<4895:CADP5S>2.0.ZU;2-8
Abstract
Racemic and enantiopure benzofuranmethanamines 5a-c have been reacted with N-Boc-3-(4-cyanophenyl)oxaziridine to give N-Boc-hydrazines 7a-c, which hav e in turn been transformed by deprotection and cyclisation into triazoles 4 a-c, potent antiaromatase agents, in good overall yield and with high enant iomeric excess. (C) 2001 Elsevier Science Ltd. All rights reserved.