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

✍ Scribed by Cameron J Cowden; Robert D Wilson*; Brian C Bishop; Ian F Cottrell; Antony J Davies; Ulf-H Dolling

• Book ID: 104211098
• Publisher: Elsevier Science
• Year: 2000
• Tongue: French
• Weight: 82 KB
• Volume: 41
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(00)01548-3

✦ Synopsis

Chlorotriazolinone 4 has been synthesised in a single step via the novel condensation of semicarbazide hydrochloride with orthoester 8. Alkylation of secondary amine 3 with compound 4 proceeds in 99% yield to afford the target NK 1 antagonist 1.