100884-47-7Relevant academic research and scientific papers
SAR of 2-benzyl-4-aminopiperidines NK1 antagonists. Part 2. Synthesis of CGP 49823
Veenstra, Siem J.,Hauser, Kathleen,Schilling, Walter,Betschart, Claudia,Ofner, Silvio
, p. 3029 - 3034 (2007/10/03)
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.
