Ramanuj Goswami

Homoenolate dianions of secondary amides via tin/lithium exchange

Abstract Treatment of N-phenyl- a well as N-methyl-3-(tri- bar|n -butylstannyl)-propionamide with 2 equiv of bar|n -butyllithium in the presence of 1,4-diazabicyclo[2.2.2]octane at −78°C in tetrahydrofuran produced the corresponding dilithio derivatives (homoenolate dianions) 4 and 8 respectively. Reaction with various electrophiles (1 equiv) gave the terminally substituted amides in good yields.

Chapter 5. Recent Advances in Neurokinin Receptor Antagonists

Publisher Summary The neurokinins, a class of peptide neurotransmitters, characterized by the common C-terminal sequence Phe-X-Gly-Leu Met-NH 2 , are widely distributed in the central and peripheral nervous systems. In this chapter, the most prominent members of the neurokinin family and their receptors are described, followed by a brief description of their physiological roles, potential therapeutic applications of neurokinin antagonists, and some of the pharmacological tools used for the study of the neurokinins. The first member of the neurokinin family to be reported was substance P (SP), which was identified as an undecapeptide. There is not yet a clear understanding of the role neurokinins play in normal physiology and in disease states, particularly in humans. They are implicated in pain and inflammation, in the immunological response, and in the central nervous system (CNS) function. One of the major advances in this field in the past several years has been the development of better pharmacological tools to aid in the study of the neurokinins. Previously, tissue preparations containing more than one receptor subtype and agonists that acted at more than one receptor subtype were used in the evaluation of potential antagonists. There are now fairly selective tissue preparations and selective potent agonists.