60 results about "Diethyl methylphosphonate" patented technology

This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme:wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.

The invention relates to a method for preparing P-[[[1-[(2-amino-9H-purine-9-yl) methyl] cyclopropyl] oxy] methyl]-phosphoric acid (Besifovir). The method comprises the following steps: 1) enabling acompound of formula (1) as shown in the specification to react with tertiary butyl diphenylchlorosilane so as to prepare a compound of formula (2) as shown in the specification; 2) enabling the compound of formula (2) to react with ethyl magnesium bromide so as to prepare a compound of formula (3) as shown in the specification; 3) enabling the compound of the formula (3) to react with p-toluenesulfonyl oxymethyldiethoxyphosphine under a condition that tertiary butanol lithium is adopted as an alkali so as to prepare a compound of formula (23) as shown in the specification; 4) carrying out ammonium fluoride hydrolysis on the compound of formula (23) so as to prepare a compound of formula (24) as shown in the specification; 5) enabling the compound of formula (24) to react with a compound offormula (28) as shown in the specification so as to prepare a compound as a solid of formula (22) as shown in the specification; 6) carrying out reduction dechloridation on the compound of formula (22) as shown in the specification under a condition of a catalyst and a hydrogen supplier so as to prepare a compound as a solid of formula (25) as shown in the specification; 7) carrying out trimethylbromide silane hydrolysis on the compound of formula (25), so as to obtain Besifovir as shown in the specification. The method is cheap in raw material and intermediate material, easy in raw materialand intermediate material obtaining, low in cost, high in yield, gentle in condition and good in security.