专利号:US-7078524-B2 优先权日:2002-11-22 标题:Process for the synthesis of ganciclovir 发明人:BABU JAYACHANDRA SURESH; RAY PURNA CHANDRA; KUMAR YATENDRA; KHANDURI CHANDRA HAS 权利人:RANBAXY LAB LTD 摘要:The present invention relates to an industrial useful process for the synthesis of antiviral compound, ganciclovir which comprises dissolving a mixture containing N-7 and N-9 isomers of structural formulae, II and III, respectively: n n nin a solvent or a mixture of solvents; separating the N-7 and N-9 isomers; and hydrolizing the N-9 isomer to obtain ganciclovir.
专利号:EP-1565469-A1 优先权日:2002-11-22 标题:Process for the synthesis of ganciclovir 发明人:BABU JAYACHANDRA SURESH; RAY PURNA CHANDRA; KUMAR YATENDRA; KHANDURI CHANDRA HAS 权利人:RANBAXY LAB LTD 摘要:The present invention relates to an industrial useful process for the synthesis of antiviral compound, ganciclovir.
专利号:WO-9724357-A1 优先权日:1995-12-28 标题 :Process for synthesis and purification of a compound useful in the preparation of acyclovir 发明人:BUEHLER HENRY J; CASKEY DOUGLAS C 权利人:MALLINCKRODT CHEMICAL INC; BUEHLER HENRY J; CASKEY DOUGLAS C 摘要:Intermediate chemical compounds useful in the preparation of acyclovir and a method of synthesizing and purifying the intermediate chemical compounds. Diacetyl-guanine is alkylated and the resulting product washed with an alcohol to produce a relatively pure, crystalline diacetyl-acyclovir (DA-ACV). The diacetyl-acyclovir (DA-ACV) is hydrolyzed in the presence of potassium hydroxide to a novel potassium salt of acyclovir, acyclovir potassium enolate. The acyclovir potassium salt is converted into essentially pure acyclovir. The step of hydrolyzing diacetyl-acyclovir and forming the potassium salt occurs simultaneously. The potassium salt of acyclovir is converted to acyclovir by dissolving in water in the presence of an acid to generate an essentially pure acyclovir. The resulting acyclovir normally needs no further purification and meets the specification of U.S.P. XXIII. Thus, the invention is directed to the synthesis of intermediate purified diacetyl-acyclovir, the conversion of the diacetyl-acyclovir to an acyclovir-potassium salt, and the conversion of the acyclovir-potassium salt to acyclovir.
专利号:US-10226434-B2 优先权日:2015-01-30 标题:Design, synthesis and methods of use of acyclic fleximer nucleoside analogues having anti-coronavirus activity 发明人:RADTKE KATHERINE L; PETERS HANNAH; NEYTS JOHAN; JOCHMANS DIRK; SNIJDER ERIC J 权利人:UNIV MARYLAND; KATHOLIEKE UNIV LEUVEN/LIEDEN UNIV MEDICAL CENTER RC LEIDEN 摘要:The present invention is directed to compounds, methods and compositions for treating or preventing viral infections using nucleosides analogs. Specifically, the present invention provides for the design and synthesis of acyclic fleximer nucleoside analogues having increased flexibility and ability to alter their conformation structures to provide increased antiviral activity potential with the result of inhibiting several coronaviruses.
专利号:US-5648489-A 优先权日:1994-05-17 标题 :Syntheses of acyclic guanine nucleosides 发明人:CHU CHUNG K; DU JINFA; WANG CHUNGUANG 权利人:UNIV GEORGIA 摘要:A method is provided for the synthesis of synthesis of acyclic purine nucleosides, particularly 9-(2-hydroxy-ethoxymethyl)-guanine (acyclovir) and 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine ('DHPG') where the N2,N9-diprotected guanine is reacted with CH3C(O)OCH2O(CH2)2)OC(O)CH3 or 2-acetoxymethoxy-1,3-diacetoxypropane, respectively, in the presence of a mixture of an acid and acetic anhydride, or in the presence of an acid, where the acid can be phosphoric acid or polyphosphoric acid.
专利号:US-6043364-A 优先权日:1996-02-22 标 题:Regiospecific process for synthesis of acyclic nucleosides 发明人:KUMAR ASHOKE; SINGH DHARMENDRA; WANI MUKESH JAGANNATH; JOSHI NARENDRA SRIRAM; THOMBRE PRAVIN SAHADEV; RAWAT AJAY SINGH 权利人:LUPIN LAB LTD 摘要:N-7 isomer of the formula is converted into a N-9 isomer of the formula by heating a suspension of the N-7 isomer in an alkylating agent of the formula