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-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-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.
专利号:EP-0998480-B1 优先权日:1997-07-25 标 题:Nucleotide analog composition and synthesis method 发明人:MUNGER JOHN D JR; 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-toluenesulfonylmethoxy-phosphonate 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.
专利号:US-7220870-B2 优先权日:1995-03-14 标 题:Hydrolytic kinetic resolution of cyclic substrates 发明人:JACOBSEN ERIC N; TOKUNAGA MAKOTO; LARROW JAY F 权利人:HARVARD COLLEGE 摘要:The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
专利号:CN-101531680-A 优先权日:2008-03-13 标 题:Synthesis of (R)-9-[2-(diethylphosphonomethoxy)propyl]-adenine