专利号:US-8193384-B2 优先权日:2005-07-29 标 题 :Polymer-bound phosphitylating reagents for the synthesis of organophosphorus compounds 发明人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF 权利人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF; RHODE ISLAND EDUCATION 摘要:The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, β-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.
专利号:WO-9407900-A1 优先权日:1992-09-25 标 题 :Synthesis of n-glycosylated compounds with the use of a mild, iodine-catalyzed reaction 发明人:KOREEDA MASATO; HOUSTON TODD A 权利人:UNIV MICHIGAN 摘要:The invention concerns N-glycosylated derivatives of nitrogen nucleophile compounds. The invention also concerns a mild, cost effective, stereoselective, regioselective, and generally applicable method for the preparation of N-glycosides by N-glycosylation of azide and amide nucleophile compounds. The method employs iodine in a catalytic amount that uniquely does not pose an environmental hazard. The invention provides efficient access to key intermediates for the synthesis inter alia of analogs of AZT and DDI and for the synthesis of conventional N-nucleoside antibiotic drugs and their novel N-glycosylated analogs.
专利号:US-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
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-6028237-A 优先权日:1996-12-16 标题:Synthesis of cyclopropylacetylene 发明人:PARSONS JR RODNEY LAWRENCE 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is a reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one which is a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
专利号:US-7205402-B2 优先权日:2004-09-02 标 题 :Synthesis of a benzoxazinone 发明人:VEMISHETTI PURUSHOTHAM; CHADWICK SCOTT T; COSTELLO CARRIE A; DESIKAN SRIDHAR; REIFF EMILY A 权利人:BRISTOL MYERS SQUIBB CO 摘要:The present invention provides novel methods for the synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (III) n nwhich is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.