FIELD: chemistry.
SUBSTANCE: present invention relates to a novel improved method of producing 5'-aminocarbonylphosphonates of nucleosides and a method of producing an acyl chloride of trimethylsilyl ether of ethoxycarbonylphosphonic acid, which is a reagent for producing 5'-aminocarbonylphosphonates of nucleosides, and can be used in pharmaceutical industry. The disclosed method involves reaction of a phosphonylating agent - acyl chloride of trimethylsilyl ether of ethoxycarbonylphosphonic acid in the presence of dimethyl formamide wiht a nucleoside with an inert aprotic solvent and treating intermediate 5'-aminocarbonylphosphonates with aqueous ammonia solution. The acyl chloride of trimethylsilyl ether of ethoxycarbonylphosphonic acid is obtained via successive treatment of triethyl phosphonoformate with trimethylbromosilane, and then with phosphorus pentachloride or thionyl chloride.
EFFECT: method of producing 5'-aminocarbonylphosphonates of nucleosides simplifies the process by using an effective reagent - acyl chloride of trimethylsilyl ether of ethoxycarbonylphosphonic acid.
2 cl, 3 ex
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