Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists

Abstract The discovery of a novel, achiral pyridine class of potent and orally active neurokinin-1 (NK 1 ) receptor antagonists is described. The evaluation of this class is briefly outlined, leading to the identification of netupitant 21 and befetupitant 29 , two new proprietary chemical entities with high affinity and excellent CNS penetration.