Study On Synthesis And Antitumor Activity Ofα-aminophosphonate Derivatives Containing Thieno [2,3-d]Pyrimidine

Thieno[2,3-d]pyrimidine is a kind of useful heterocyclic compound, which contains sulfur and nitrogen atoms simultaneously, In drug screening and development, the derivatives of thieno[2,3-d]pyrimidine play an important role because of their diverse biological activities, such as antitumor, antiviral, antimicrobial, anti-inflammatory, analgesic, antimalarial, antiproliferation and so on. a-Aminophosphonate derivatives also have attracted many attentions and widely used in pharmaceuticals and agricultural fields, since they could be antitumor, antibiotics, herbicides and enzyme inhibitors.Then, based on the principle of bioactive superposition, we introduced the thieno[2,3-d]pyrimidine ring into a-aminophosphonate compounds. Consequently, twenty-two a-aminophosphonate derivatives (6ma～6mk and6na～6nk) were synthesized. All these thirty-three compounds, including intermediates4a-4k have not been reported in literature. The structures of all compounds were characterized by31P NMR,1H NMR,13C NMR, IR, MS or HRMS. At the same time, antitumor activity of some target compounds and intermediates were determined preliminarily.The synthetic route is shown in Scheme1.