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-5214134-A 优先权日:1990-09-12 标题:Process of linking nucleosides with a siloxane bridge 发明人:WEIS ALEXANDER LUDVIK; SAHA ASHIS KUMAR; HAUSHEER FREDERICK HERMAN 权利人:STERLING WINTHROP INC 摘要:A method of linking nucleosides with a siloxane bridge comprising reacting a 3'-silylated-5'-protected nucleoside with an unprotected nucleoside is disclosed. The silylated and unprotected nucleosides may be either monomeric nucleosides or the terminal nucleosides of an oligonucleotide or oligonucleotide analog. A method of synthesizing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed. The method of synthesis comprises silylating a 5'-protected nucleoside with a bifunctional silylating reagent to form a 3'-silylated nucleoside, reacting the silylated nucleoside with an unprotected nucleoside in the presence of a base catalyst and repeating these steps to form an oligonucleotide analog. A modified solid phase synthesis method for preparing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed.
专利号:JP-2003513984-A 优先权日:1999-11-12 标题 :Synthesis of 2'-deoxy-L-nucleoside
专利号:US-2011009606-A1 优先权日:2009-01-15 标题:Synthesis of 2',3' - and 3',5' -cyclic phosphate mono-and oligonucleotides
专利号:EP-1179598-B1 优先权日:1999-05-13 标题 :Process for producing nucleoside compound 发明人:NIKUMARU SEIYA; NAKAMURA TAKESHI 权利人:MITSUI CHEMICALS INC 摘要:In preparation of a nucleoside compound by reacting a pentose-1-phosphate and a nucleic acid base or its analogue in the presence of enzyme activity of nucleoside phosphorylase, a metal salt capable of forming a water-insoluble salt with phosphoric acid may be added to a reaction system to eliminate phosphoric acid, a byproduct, from the reaction system so that the equilibrium reaction can be shifted toward a direction for nucleoside synthesis, leading to an improved yield of the desired nucleoside compound.
[参考文献]: A S Jones, Et Al. A Method For The Rapid Preparation Of 5-Vinyluracil In High Yield. Nucleic Acids Res. 1974 Jan;1(1):105-7. [参考文献]: Kazuo Hattori, Et Al. Design And Synthesis Of The Tumor-Activated Prodrug Of Dihydropyrimidine Dehydrogenase (Dpd) Inhibitor, Ro0094889 For Combination Therapy With Capecitabine. Bioorg Med Chem Lett. 2003 Mar 10;13(5):867-72.