Abstract
New cyclophosphamide derivatives having the 1, 3, 4, 2-oxadiazaphosphorinane and related heterocyclic systems were prepared by the ozonolysis reactions of O-(2-propenyl)-and O-(3-butenyl)-N, N-bis(2-chloroethyl) phosphoramidoyl hydrazides and their derivatives. The newly synthesized heterocyclic systems were dihydro-6H-1, 3, 4, 2-oxadiazaphos-phorine-2-oxide, 4-acetyl-5-hydroxy-1, 3, 4, 2-oxadiazaphosphorinane-2-oxide, 4-acetyl-5-hydroxyhexahydro-2H-1, 3, 4, 2-oxadiazaphosphepine-2-oxide and perhydro-1, 3, 4-oxadiazolo [3, 2-c]-1, 3, 2-oxazaphosphorine-1-oxide. Comparative studies of the in vivo antileukemic activity revealed that these cyclophosphamide derivatives were ineffective in promoting the antitumor action.
