Title of article
SAR of 2-benzyl-4-aminopiperidines NK1 antagonists. Part 21. synthesis of CGP 49823
Author/Authors
Siem J. Veenstra، نويسنده , , Kathleen Hauser، نويسنده , , Walter Schilling، نويسنده , , Claudia Betschart، نويسنده , , Silvio Ofner، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1996
Pages
6
From page
3029
To page
3034
Abstract
CGP 49823 is a potent NK1 antagonist which is centrally active after oral administration. The SAR of the C-2 substituent was investigated with respect to the affinity to the NK1 receptor. A practical synthesis of CGP 49823, suitable for scale-up, was developed. The key-step, a tandem acyliminium ion cyclization / Ritter reaction, gave trans 2-benzyl-4-acetamido-piperidines with high diastereoselectivity.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1996
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
788491
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