专利号:US-5591852-A 优先权日:1990-08-10 标题 :Process for the preparation of nucleotides 发明人:VEMISHETTI PURUSHOTHAM; BRODFUEHRER PAUL R; HOWELL HENRY G; SAPINO JR CHESTER 权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING 摘要:The present invention relates to a novel and economical process for the synthesis of HPMP-substituted nucleotide antiviral compounds. Also disclosed are novel intermediates produced in the process for the preparation of HPMPC.
专利号:US-10155007-B2 优先权日:2014-10-29 标 题:Synthesis method for improved tenofovir disoproxil fumarate using ion-exchange resin and method for preparing oral dissolving film form using the same 发明人:KIM DONG-JIN; KOO CHANG-HUI; CHO IL-HEE; LEE SUNG-BAE; HAN DONG-HOON 权利人:FIRSON 摘要:The present invention relates to a synthesis method of preventing the formation of impurities and byproducts in the synthesis of tenofovir disoproxil fumarate (Teno-DF) used as a medicine for hepatitis B and HIV treatment due to its function to promote bioactivities. In the synthesis method of the present invention, an ion-exchange resin (Dowex 50W hydrogen form, sulfonic acidic cation exchange resin) is used to enhance the yield and purity of the compound. The present invention also relates to a method of preparing an oral dissolving film dosage form in the manufacture of a medicine using the tenofovir compound with high purity obtained by the synthesis method of the present invention as an effective ingredient.
专利号:US-9303051-B2 优先权日:2010-08-31 标 题 :Phosphonate ester derivatives and methods of synthesis thereof 发明人:WARE ROY W; ALMOND MERRICK R; LAMPERT BERNHARD M 权利人:CHIMERIX INC; CHIMERIX INC 摘要:The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.
专利号:US-2018111938-A1 优先权日:2015-05-05 标 题:Synthesis of Intermediates Used in the Manufacture of Anti-HIV Agents 发明人:PRADHAN BRAJA SUNDAR; AMARNATH KOMMIREDDY; VEMPALA NARESH; RAHMAN MD ATAUR 权利人:CBZ INVEST LTD 摘要:The present invention relates to a process of preparing intermediates of Formula (I). The process comprises of reacting compound of Formula (III) with compound of Formula (V) in the presence of a solvent selected from an alcohol, ether or water to form compound of Formula (I) wherein, R 1 is selected from —NH 2 , Cl, Br, NHCOR″, wherein R″ is alkyl, aryl, Schiff's base of formula Nâ•?CHR′, wherein R′ is alkyl or aryl; R 2 is selected from H, alkyl; R 3 and R 4 , each independently is H; R 5 and R 6 , each independently is H, alkyl; R 7 is H, alkyl; and R 8 is H, alkyl.
专利号:US-2017029451-A1 优先权日:2013-12-05 标 题:Branched chain acyclic nucleoside phosphonate esters and methods of synthesis and uses thereof 发明人:WARE ROY W; DOWNEY AARON L; LANIER ERNEST RANDALL; SETHNA PHIROZE; SELLESETH DEAN 权利人:CHIMERIX INC 摘要:The present invention is directed to branched chain nucleoside phosphonate ester compounds and methods of synthesis thereof. The present invention is also directed to pharmaceutical compositions comprising branched chain nucleoside phosphonate ester compounds and methods of treating and/or preventing double stranded DNA viral infection and/or viral infection associated disease or disorder.
专利号:US-5935946-A 优先权日:1997-07-25 标 题 :Nucleotide analog composition and synthesis method 发明人:MUNGER JR JOHN D; ROHLOFF JOHN C; SCHULTZE LISA M 权利人:GILEAD SCIENCES INC 摘要:The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p-toluenesulfonylmethoxyphosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.