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.

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 and anticancer activity of 2-substituted 2,3-dihydro-1,3,2- benzoxazaphosphorin-4-one and its 2-oxide derivatives.

As a result of the reaction of salicylic amide with PCl3 and POCl3 2-chloro-2,3-dihydro-1,3,2-benzoxazaphosphorin-4-one (1) and its 2-oxide 2 are obtained. Compounds 1 and 2 form amides with amines in 2-position. Antineoplastic action of the derivatives containing the bis(2-chloroethyl)amide group in 2-position was found.

[Synthesis and pharmacologic examination of derivatives of benzoxazaphosphoryl-4-one and 2-phenyl-10-methyl-3a-triethoxyphosphone-1H,2,3,9,10-tetrahydropyrrolo [3,4-b][1,4]benzoxazepine-1,3,9-trione]. / Synteza i badania farmakologiczne pochodnych benzoksazafosforyno-4-on i 2-fenylo-10-metylo-3a-trietoksyfosfonio-1H,2,3,9,10-tetrahydropirolo [3,4-b][1,4] benzoksazepino-1,3,9-trionu.

A series of N-derivatives of 2-phenyl-2,3-dihydro-1,3,2(lambda 5)- benzoxazaphosphoryl-4-one and 2-phenyl-10-methyl-3a-triethoxyphosphonio- 1H,2,3,9,10-tetrahydropyrrolo[3,4-b]([1,4]benzoxazepine-1,3,9-trio ne have been prepared. The pharmacological investigation of the above mentioned compounds shows antitumor action against leukaemia in the case of three N-derivatives.

[Synthesis and cytostatic effect of 2-phenyl-3-alkyl(aryl)-2,3-dihydro-1,3,2(lambda-5)- benzoxazaphosphorine-4-one derivatives]. / Synthese und zytostatische Wirkung einiger 2-phenyl-3-alkyl(aryl)-2,3-dihydro-1,3,2(lambda 5)-benzoxazaphosphorin-4-on- derivate.

Preparation of 2,3-dihydro-1,3,2-benzoxazaphosphorin-4-one derivatives and their 2-oxo derivatives is described. Compounds 1 and 12 have anticancer activity.