Analysis of crucial structural requirements of 2-substituted pyrimido[4,5-b][1,5]oxazocines as NK1 receptor antagonist by axially chiral derivatives

This study aimed to identify the crucial structural features of 2-substituted 8-methylpyrimido[4,5-b][1,5]oxazocine derivatives. Axially chiral 8-methylpyrimido[4,5-b][1,5]oxazocines bearing a substituent at the C-2 position were synthesized and evaluated as NK1 antagonists. The results revealed that (aR, 8S)-stereochemistry and the substituent at the C-2 position are important for NK1 receptor recognition.

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