专利号:US-2004242897-A1 优先权日:2002-07-31 标题 :Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are 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:US-9783549-B2 优先权日:2013-11-04 标题:Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E; LEE JAEMOON 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
专利号:WO-2004011474-A1 优先权日:2002-07-31 标题:Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-6653468-B1 优先权日:2002-07-31 标 题 :Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 权利人:ISIS PHARMACEUTICALS INC 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-4780504-A 优先权日:1985-06-20 标 题 :Supports useful in solid phase synthesis of oligonucleotides 发明人:BUENDIA JEAN; NIERAT JEANINE 权利人:ROUSSEL UCLAF 摘要:Novel supports useful in solid phase synthesis of oligonucleotides of the formula I +TR wherein &cir& is micro pellets of a material selected from the group consisting of glass, silica, Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkylene of 1 to 20 carbon atoms, saturated cycloalkylene of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x is an integer from 0 to 20, x1 is an integer from 0 to 10 and the amino group may be in the m-, p- or o-position, a process for the preparation of said supports, the use of said supports and intermediates.