CAS: 201341-05-1; (R)-(((((1-(6-Amino-9H-Purin-9-yl)Propan-2-yl)Oxy)Methyl)Phosphoryl)Bis(Oxy))Bis(Methylene) Diisopropyl Dicarbonate

上下游产品

chloromethyl isopropyl carbonate tenofovir 4-dimethylaminomethylideno-9-(2-phosphonomethoxypropyl)adenine bis(isopropyloxycarbonyloxymethyl) ester(R)-N4-dimethylaminomethylideno-9-(2-phosphonomethoxypropyl)adenine bis(isopropyloxycarbonyloxymethyl) ester adeninetenofovir tenofovir disoproxil hemifumarate Tenofovir mono-P°C 20H32N5O11PC20H32N5O11P

泰诺福韦置于三乙胺,氯甲基碳酸异丙酯,氨体系中,用 环己烷,N-甲基吡咯烷酮,水 用作溶剂,化学反应 6.0H,反应生成替诺福韦酯
参考文献: Process For The Preparation Of Tenofovir[fr] Procédé De Synthèse Du Ténofovir
标题: Process For The Preparation Of Tenofovir[fr] Procédé De Synthèse Du Ténofovir
摘要:本发明提供了一种制备替诺福韦的方法.本发明还提供了一种制备替诺福韦二丙氧基醇盐或其盐的方法,以及使用本发明的替诺福韦制备其药物组合物的方法.

专利信息

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:EP-1543168-B1
优先权日:2002-09-27
标 题:Method for assaying replication of hbv and testing susceptibility to drugs
发明人：DURANTEL DAVID; DURANTEL SANDRA; TREPO CHRISTIAN; ZOULIM FABIEN
权利人:INST NAT SANTE RECH MED
摘要:Measuring the replication capacity of hepatitis B virus (HBV), e.g. HBV in a biological sample, possibly in the presence of a pharmaceutical product, and particularly an antiviral agent, is new. Measuring the replication capacity of hepatitis B virus (HBV), e.g. HBV present in a biological sample, possibly in the presence of a pharmaceutical product, particularly an antiviral agent, comprises: (a) optional extraction of nucleic acids contained in the sample; (b) PCR amplification of HBV nucleic acids using at least 2 primer pairs to obtain at least 2 amplified HBV genomic fragments representing more-than-full-length HBV genome; (c) cloning the fragments obtained into a vector; (d) transfecting or transducing susceptible cells with the vector; (e) culturing the transfected or transduced cells in conditions allowing synthesis of HBV pregenomic RNA (pgRNA) from the cloned HBV DNA; (f) optionally treating the cultured cells with a pharmaceutical product, particularly an antiviral agent; and (g) determining the replication capacity of the HBV, and the effect of any pharmaceutical product used on viral gene expression and/or viral replication. Independent claims are also included for: (1) a polynucleotide useful as primer for HBV amplification, comprising a sequence selected from 21 sequences of 23-42 bp (SEQ ID NO: 1-21) given in the specification; (2) a primer pair for HBV amplification comprising: (a) a forward primer comprising SEQ ID NO: 1-12, and/or a reverse primer comprising SEQ ID NO: 13 or SEQ ID NO: 14; (b) a forward primer comprising SEQ ID NO: 15 and/or 16 or 19, and a reverse primer comprising SEQ ID NO: 17 and/or SEQ ID NO: 18; (c) a forward primer comprising SEQ ID NO: 19, and a reverse primer comprising SEQ ID NO: 17 and/or SEQ ID NO: 18; or (d) a forward primer comprising SEQ ID NO: 20 or 22, and a reverse primer comprising SEQ ID NO: 21 or 23; (3) kits for HBV amplification, comprising a primer pair of (2); (4) a vector comprising a more-than-full length HBV genome as defined above, and a promoter modified in the 5' by the presence of a restriction site in the 5' of the +1 of transcription, where the +1 of transcription of the more-than-full length HBV genome and of the promoter are fused, and the promoter controls the synthesis of a pgRNA from the more-than-full length HBV genome post-cell-transfection; and (5) a baculovirus or cell line comprising the vector. ACTIVITY : Virucide. MECHANISM OF ACTION : None given.

专利号:US-2016185745-A1
优先权日:2013-08-07
标题:Analogs of vinaxanthone and xanthofulvin, methods of synthesis, and methods of treatments thereof
发明人：SIEGEL DIONICIO; CHIN MATTHEW; ELIASEN ANDERS; AXELROD ABRAM
权利人:UNIV TEXAS
摘要:The present invention relates generally to methods of synthesis of vinaxanthone and xanthofulvin, novel analogs, and methods of use thereof.

专利号:WO-2016202721-A1
优先权日:2015-06-16
标 题:Salts of (s)-4-[(r)-6-(2-chloro-4-fluoro-phenyl)-5-methoxycarbonyl-2-thiazol-2-yl-3,6- dihydro-pyrimidin-4-ylmethyl]-morpholine-3-carboxylic acid, salt former and methods for preparing and using the same
发明人：EGLI ANDRé; DIODONE RALPH; WUITSCHIK GEORG
权利人:HOFFMANN LA ROCHE; HOFFMANN LA ROCHE
摘要:The present invention relates to salts of (S)-4-[(R)-6-(2-Chloro-4-fluoro-phenyl)-5- methoxycarbonyl-2-thiazol-2-yl-3,6-dihydro-pyrimidin-4-ylmethyl]-morpholine-3-carboxylic acid and an acid, the synthesis of the acid salts, and their use for the treatment of pathological disorders, particularly hepatitis B (HBV) infection.

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.