Synthesis of N4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy ] -3-oxo-5-pyrido [1, 4] oxazin-6-yl)-5-fluoro-N2- (3, 4, 5,-trimethoxyphenyl) -2, 4- pyrimidinediamine disodium salt

摘要

This invention relates to the field of pharmaceutical/process chemistry. Disclosed herein is a process for preparing N4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy) methyl] -3-oxo-5-pyrido [1,4] oxazin-6-yl) -5~fluoro-N2- (3,4, 5-trimethox yphenyl) -2, 4-pyrimidinediamine disodium salt, particularly hydrates (such as a hexahydrate). The compound is useful in the treatment and prevention of various diseases. Also disclosed is a process of preparing N4- (2, 2-dimethyl-4- [ (dialkyl phosphonoxy) methyl] -3-oxo-5-pyrido [1, 4] oxazin-6-yl) -5-f luoro-N2- (3,4, 5-trimethox yphenyl ) -2, 4-pyrimidinediamine. Both processes involve the use of an amide. in.