A new synthesis of 1,2,4-triazolin-5-ones: application to the convergent synthesis of an NK1 antagonist

Authors
Cowden, CJ Wilson, RD Bishop, BC Cottrell, IF Davies, AJ Dolling, UH
Citation
Cj. Cowden et al., A new synthesis of 1,2,4-triazolin-5-ones: application to the convergent synthesis of an NK1 antagonist, TETRAHEDR L, 41(44), 2000, pp. 8661-8664
Citations number
12
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON LETTERS
ISSN journal
00404039 → ACNP
Volume
41
Issue
44
Year of publication
2000
Pages
8661 - 8664
Database
ISI
SICI code
0040-4039(20001028)41:44<8661:ANSO1A>2.0.ZU;2-8
Abstract
Chlorotriazolinone 4 has been synthesised in a single step via the novel co ndensation of semicarbazide hydrochloride with orthoester 8. Alkylation of secondary amine 3 with compound 4 proceeds in 99% yield to afford the targe t NK, antagonist 1. (C) 2000 Published by Elsevier Science Ltd.