专利号:US-5856465-A 优先权日:1996-05-24 标 题:Compositions and methods for the synthesis of chirally pure organophosphorus nucleoside derivatives 发明人:STEC WOJCIECH JACEK; WOZNIAK LUCYNA 权利人:POLSKA AKAD NAUK CENTRUM 摘要:Methods for the stereospecific synthesis of chirally pure organophosphorus dinucleotide derivatives and nucleoside monomer synthons used in their synthesis are provided. These methods allow for conversion of nucleoside intermediates of unchosen sense of P-chirality to nucleoside monomer synthons of chosen sense of P-chirality. Also provided are novel nucleoside intermediates useful in such methods.
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-5204456-A 优先权日:1986-04-08 标题:Derivatives of nucleosides and their use for the synthesis of oligonucleotides 发明人:MOLKO DIDIER; SCHULHOF JEAN-CLAUDE; TEOULE ROBERT 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:The invention relates to derivatives of nucleosides and their use for the synthesis of oligonucleotides. These derivatives are in accordance with the formula: (I) in which B represents a radical derived from guanine, cytosine or adenine, whose exocylic NH group is protected by the group with R1 representing a hydrogen atom or a alkyl radical and R2 a hydrogen atom, and alkyl radical, an alkoxy radical and optionally substituted aryloxy radical, R3 represents a hydrogen atom, the dimethoxytrityl radical or the radical R4 represents a hydrogen atom, the radical of formula: or a radical suitable for the synthesis of polynucelotides and R5 represents a hydrogen atom or the protected or unprotected hydroxyl OH radical.
专利号:EP-0850248-B1 优先权日:1995-09-01 标 题 :Compositions and methods for the synthesis of organophosphorus derivatives 发明人:STEC WOJCIECH J; WOZNIAK LUCYNA 权利人:POLSKA AKAD NAUK CENTRUM 摘要:Methods for the stereospecific synthesis of chirally pure organophosphorus dinucleotide derivatives and nucleoside monomer synthons used in their synthesis are provided. These methods allow for conversion of nucleoside intermediates of unchosen sense of P-chirality to nucleoside monomer synthons of chosen sense of P-chirality. Also provided are novel nucleoside intermediates useful in such methods.
专利号:US-6262251-B1 优先权日:1995-10-19 标题 :Method for solution phase synthesis of oligonucleotides 发明人:PIEKEN WOLFGANG; MCGEE DANNY; SETTLE ALECIA; ZHAI YANSHENG; HUANG JIANPING 权利人:PROLIGO LLC 摘要:This invention discloses an improved method for the sequential solution phase synthesis of oligonucleotides. The method lends itself to automation and is ideally suited for large scale manufacture of oligonucleotides with high efficiency.
专利号:WO-9847910-A1 优先权日:1997-04-21 标题:Method for solution phase synthesis of oligonucleotides 发明人:PIEKEN WOLFGANG; MCGEE DANNY; SETTLE ALECIA; ZHAI YANSHENG; HUANG JIANPING; HILL KEN; SMITH RANDALL S 权利人:NEXSTAR PHARMACEUTICALS INC; PIEKEN WOLFGANG; MCGEE DANNY; SETTLE ALECIA; ZHAI YANSHENG; HUANG JIANPING; HILL KEN; SMITH RANDALL S 摘要:This invention discloses an improved method for the sequential solution phase synthesis of oligonucleotides. The method lends itself to automation and is ideally suited for large scale manufacture oligonucleotides with high efficiency.
参考标题:Sequential 1,3-N- To C- And 1,3-C- To C-Migration Of Sulfonyl Groups Through The Synthesis Of 1,4-Diazepines From The Aza-[5 + 2] Cycloaddition Of Indoloazomethine Ylides 作者:Namrim Heo,Ilyong Jung,Dae Kyum Kim,Sang Hoon Han,Kooyeon Lee,Phil Ho Lee |发布日期:2020.8.21 摘要:Sequential 1,3-N- To C- And 1,3-C- To C-Migration Of Sulfonyl Groups Through The Synthesis Of 1,4-Diazepines From An Operationally Simple Thermal Aza-[5 + 2] Cycloaddition Reaction Of Indoloazomethine Ylides With Dialkyl Acetylenedicarboxylates Under Mild Conditions, Leading To The Formation Of C-Sulfonylated 1,4-Diazepines.
合成参考文献
参考文献:10.1007/978-1-61779-188-8_3 摘要:Hari Y, Kodama T, Imanishi T, Obika S. 2'-O,4'-C-methyleneoxymethylene bridged nucleic acids (2',4'-BNA(COC)). Methods Mol Biol. 2011;764():31–57. doi: 10.1007/978-1-61779-188-8_3.