Synthesis and Action on the Central Nervous System of 3‐Substituted 2‐Phenyl‐2,3‐dihydro‐4H‐1,3,2‐benzoxazaphosphorin‐4‐one 2‐Oxide and 2‐Sulfide Derivatives

Abstract

The synthesis of 3-substituted 2-phenyl-2,3-dihydro-4H-1,3,2-benzoxazaphosphorin-4-one 2-sulfide derivatives is described. The action of a series 2-oxide (1-6) and 2-sulfide (7-12) derivatives on the central nervous system has been evaluated. Compounds 1-4, 6, 7-10 exhibit neuroleptic activity. Derivatives of sulfide series act as antiserotoninergic drugs.

Synthesis of some pyrazolo[1,5-c][1,3]benzoxazines and a new 5H-pyrazolo[1,5-c][1,3,2]benzoxazaphosphorine ring system

“…Considering that some 1,3,2-benzoxazaphosphorines exhibit interesting anticancer [19] and neuroleptic [20] properties and act as antiserotoninergic drugs [20], derivative 8 might be a valuable bioactive molecule.…”