CAS: 202138-50-9; (R)-(((((1-(6-Amino-9H-Purin-9-yl)Propan-2-yl)Oxy)Methyl)Phosphoryl)Bis(Oxy))Bis(Methylene) Diisopropyl Dicarbonate Fumarate

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CAS号35180-01-9 氯甲基异丙基碳酸酯 | CAS号110-17-8 富马酸,反丁烯二酸 | CAS号147127-20-6 泰诺福韦 | CAS号1215085-38-3 tenofovir disop... | CAS号14047-28-0 (R)-9-(2-羟基丙基)腺嘌呤 | CAS号180587-75-1 (R)-9-[2-(二乙基膦酰... | CAS号66224-66-6 6H-Purin-6-imin...

泰诺福韦置于三乙胺体系中,用 N-甲基吡咯烷酮,环己烷 用作溶剂,化学反应 6.17H,反应生成富马酸替诺福韦酯
参考文献: An Improved Process For The Preparation Of Tenofovir Disoproxil And Pharmaceutically Acceptable Salts Thereof[fr] Procédé Amélioré Pour La Préparation De Ténofovir Disoproxil Et Des Sels Pharmaceutiquement Acceptables De Celui-Ci
标题: An Improved Process For The Preparation Of Tenofovir Disoproxil And Pharmaceutically Acceptable Salts Thereof[fr] Procédé Amélioré Pour La Préparation De Ténofovir Disoproxil Et Des Sels Pharmaceutiquement Acceptables De Celui-Ci
摘要:一种改进的tenofovir Disoproxil及其药用可接受盐的制备方法,包括以下步骤:A)用(R)-4-甲基-1,3-二氧杂环己-2-酮烷基化腺嘌呤,分离(R)-1-(6-氨基-9H-嘌呤-9-Yl)丙-2-醇;B)用二烷基对甲苯磺酰氧甲基膦酸酯或二烷基卤代甲基膦酸酯烷基化(R)-1-(6-氨基-9H-嘌呤-9-Yl)丙-2-醇,得到(R)-9-[2-(磷酸甲氧基)丙基]腺嘌呤的二烷基酯;C)通过微波辐射下的矿酸去烷基化磷酸酯基团制备(R)-9-[2-(磷酸甲氧基)丙基]腺嘌呤((R)-Pmpa; Tenofovir);D)制备tenofovir Disoproxil;E)制备tenofovir Disoproxil的富马酸盐或其他药用可接受盐.

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-9206209-B2
优先权日:2010-10-19
标 题:Nucleotide analogue, method of synthesis of nucleotide analogue, use of nucleotide analogue, antiviral pro-nucleotide, pharmaceutical composition
发明人：KRASZEWSKI ADAM; ROMANOWSKA JOANNA; SOBKOWSKI MICHAL; SZYMANSKA-MICHALAK AGNIESZKA; STAWINSKI JACEK; BORYSKI JERZY; LIPNIACKI ANDRZEJ; PIASEK ANDRZEJ
权利人:KRASZEWSKI ADAM; ROMANOWSKA JOANNA; SOBKOWSKI MICHAL; SZYMANSKA-MICHALAK AGNIESZKA; STAWINSKI JACEK; BORYSKI JERZY; LIPNIACKI ANDRZEJ; PIASEK ANDRZEJ; INST CHEMII BIOORG PAN; NARODOWY INST LEKOW
摘要:An exemplary emboidment is related to a pharmaceutical composition of the class of nucleotide analogues and antiviral pro-nucleotides useful in partial or complete inhibition of human immunodeficiency virus (HIV). An exemplary embodiment is expressed in the formula (XVI): n nwhere X stands for N 3 and B stands for thymidine-1-yl, or X stands for H and B stands for uracil-1-yl or adenin-1-yl or hypoxanthin-1-yl.A method of synthesis of the nucleotide analogue using a phosphorylating agent for synthesis of the nucleotide analogue is provided.

专利号:US-8278483-B2
优先权日:2006-02-07
标题:Process for synthesis of glycomimicking cationic amphiphiles
发明人：MAHIDHAR YENUGONDA VENKATA; CHAUDHURI ARABINDA; MUKHERJEE RAMA
权利人:MAHIDHAR YENUGONDA VENKATA; CHAUDHURI ARABINDA; MUKHERJEE RAMA; COUNCIL SCIENT IND RES
摘要:The present invention provides processes for the synthesis of novel Shikimic acid head-group containing non-toxic cationic amphiphiles capable of facilitating transport of biological macromolecules into cells.

专利号:US-2025090698-A1
优先权日:2018-11-27
标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases
发明人：CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT
权利人:INDIAN INSTITUTE OF TECH INDORE
摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.

专利号:US-9334273-B1
优先权日:2014-03-05
标题:Efficient and stereoselective synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA)
发明人：CHU DAVID C K; SINGH UMA S
权利人:UNIV GEORGIA
摘要:The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) from a readily available starting material (Vince lactam) in fourteen steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, D -2′-fluoro-6′-methylene cyclopentanol by diazotization, elimination, stereoselective epoxidation, fluorination and oxidative reduction of the Vince lactam in twelve steps is also provided.

专利号:US-7582758-B2
优先权日:2004-06-08
标 题:Lewis acid mediated synthesis of cyclic esters
发明人：MARTIN KEVIN V
权利人:METABASIS THERAPEUTICS INC
摘要:Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.