Synthesis and formulations of salts of isophosphoramide mustard and analogs thereof

摘要

Disclosed herein are formulations and methods of manufacture of compounds of formula (E):;
wherein X and Y independently represent leaving groups; and A+ is an ammonium cation.

主权项

1. A method for the preparation of a compound of formula (D):comprising treating a compound of formula (C):under hydrogenolysis conditions, wherein as valence and stability permit,
X and Y independently represent leaving groups; R1 is benzyl optionally substituted with one or more substituents selected from halogen, —R2, —OR2 and —NR22 wherein R2 is selected in each occurrence from H and lower alkyl; and the hydrogenolysis condition comprises a solvent system comprising one or more aprotic organic solvents.