专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-2024287520-A1 优先权日:2021-06-30 标题:Method for synthesis of linkage modified oligomeric compounds 发明人:RODRIGUEZ ANDREW A 权利人:IONIS PHARMACEUTICALS INC 摘要:The present disclosure provides methods of synthesizing modified oligonucletodies and oligomeric compounds (including oligomeric compounds that are antisense agents or portions thereof) comprising a modified oligonucleotide having at least one modified internucleoside linking group. In certain embodiments, the present disclosure provides stabilized formulations of certain sulfonyl azides for use in the synthesis of olignonucleotides comprising one or more sulfonyl phosphoramidate linkages. Some embodiments provide stabilized compositions of high energy reagents that may be used in the synthesis of modified oligonucleotides, allowing for safe process scale preparation thereof.
专利号:US-11434211-B2 优先权日:2020-06-16 标题:Synthesis of 5-nitrotetrazole 发明人:PIERCEY DAVIN GLENN; MANSHIP TIMOTHY D; SMITH DAWSON MICHAEL 权利人:PURDUE RESEARCH FOUNDATION 摘要:This disclosure shows the ability of a readily-available oxidizer to achieve oxidation of 5-amino-1H-tetrazole (5-AT) to 5-nitrotetrazole (5-NT) in high yields in a single pot synthesis. This strategy reduces the synthesis of this important energetic material down to a single step and eliminates highly sensitive diazonium and copper salt primary explosive intermediates. The overall yield of this process is 48-53% and the resultant aqueous solution of product effectively used for the preparation of nitrotetrazole-containing primary explosive DBX-1. Unlike current methods of nitrotetrazole preparation, the novel method is entirely solution-based and prepares a final solution of sodium nitrotetrazolate, never once needing to handle energetic intermediates or products, making it a much safer method of nitrotetrazole preparation.
专利号:US-5442065-A 优先权日:1993-09-09 标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin 发明人:MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A 权利人:UNIV TEXAS 摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.
专利号:WO-2013091696-A1 优先权日:2011-12-21 标题 :Synthesis of intermediates for preparing anacetrapib and derivatives thereof 发明人:HUMLJAN JAN; MARAS NENAD 权利人:LEK PHARMACEUTICALS; HUMLJAN JAN; MARAS NENAD 摘要:The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.
专利号:US-4347379-A 优先权日:1980-03-10 标 题:Synthesis of alpha-alkoxycarboxylic acids 发明人:LAI JOHN T 权利人:GOODRICH CO B F 摘要:Numerous alpha-carboxylic acids are prepared in a liquid medium by the reaction of an organic compound having at least one reactive hydroxyl or thiol group, with a monoketone, and a haloform, in the presence of a phase transfer catalyst and an alkali metal hydroxide. The term 'alpha-alkoxycarboxylic acids' includes alpha-phenoxycarboxylic acids, alpha-thioalkoxycarboxylic acids and alpha-thiophenoxycarboxylic acids. Specific substituents on the beta carbon atom of an alpha-alkoxycarboxylic (or '2-alkoxycarboxylic') acid reaction product formed in this novel synthesis, are introduced by appropriate choice of the ketone reactant; alkoxy and phenoxy substituents on the alpha carbon atom of a 2-alkoxycarboxylic acid are introduced by appropriate choice of the organic compound having a hydroxyl or thiol group. De-alkoxylation of the 2-alkoxycarboxylic acid yields alpha-beta monoolefinically unsaturated carboxylic acids which are necessarily alpha substituted, and may also be beta-substituted. It is now possible to produce, simply and conveniently, numerous substituted alpha-beta monolefinically unsaturated carboxylic acids with a variety of substituents on the alpha carbon atom, and, optionally on the beta carbon atom of these substituted carboxylic acids. Esters may also be conventionally derived from both the 2-alkoxycarboxylic acids, and the unsaturated carboxylic acids. During the phase transfer catalyzed synthesis of this invention, an intermediate acyl halide derivative is formed prior to the formation of the 2-alkoxycarboxylic acid reaction product. The formation of the acyl halide derivative allows the subsequent direct formation, in a modification of the same reaction, of 2-alkoxycarboxylic acid amides (or '2-alkoxycarbamides'), simply by adding a primary or secondary amine to the reaction mass. By dealkoxylation of the 2-alkoxycarbamides, specific, necessarily alpha-substituted and optionally beta-substituted acrylamides are synthesized which previously could be prepared, if at all, only with difficulty.
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合成参考文献
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