专利号:US-11518780-B2 优先权日:2019-07-31 标 题:Sensitive oligonucleotide synthesis using sulfur-based functions as protecting groups and linkers 发明人:FANG SHIYUE 权利人:FANG SHIYUE 摘要:Embodiments for the synthesis of sensitive oligonucleotides as well as insensitive oligonucleotides are provided. Sulfur-based groups are used for the protection of exo-amino groups of nucleobases, phosphate groups and 2′—OH groups, and as cleavable linker for linking oligonucleotides to a support. Oligonucleotide syntheses are achieved under typical conditions using phosphoramidite chemistry with important modifications. To prevent replacing sulfur-based protecting groups by acyl groups via cap-exchange, special capping agents are used. To retain hydrophobic tag to assist RP HPLC purification, special phosphoramidites are used in the last synthetic cycle. With the sulfur-based groups for protection and linking, oligonucleotide deprotection and cleavage are achieved via oxidation followed by beta-elimination under mild conditions. Therefore, besides for insensitive oligonucleotide synthesis, the embodiments of the invention are capable for the synthesis of oligonucleotide analogs containing sensitive functional groups that cannot survive the harsh conditions used in prior art oligonucleotide synthesis technologies.
专利号:US-9751851-B2 优先权日:2013-09-20 标 题:Molecules and compositions that inhibit gram negative bacteria and their uses 发明人:BASSLER BONNIE L; SEMMELHACK MARTIN F; DRESCHER KNUT; SIRYAPORN ALBERT; CONRAD-MILLER LAURA C; O'LOUGHLIN COLLEEN T 权利人:UNIV PRINCETON; BASSLER BONNIE L; SEMMELHACK MARTIN F; DRESCHER KNUT; SIRYAPORN ALBERT; MILLER LAURA C; O'LOUGHLIN COLLEEN T 摘要:Antivirulence strategies to combat Pseudomonas aeruginosa , are described. One strategy encompasses synthesis of a series of compounds that inhibit the production of pyocyanin, a redox-active virulence factor produced by this pathogen. A related strategy encompasses synthesis of compounds that inhibit the two P. aeruginosa quorum-sensing receptors, LasR and RhlR, inhibit production of pyocyanin, and inhibit biofilm formation.
专利号:US-5130478-A 优先权日:1989-12-06 标题:Process for the preparation of chlorides of chlorinated carboxylic acids 发明人:GAUTHIER PATRICIA P; LE MOULT MICHEL M; ROCHELLE CLAUDE; SENET JEAN-PIERRE G 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The invention relates to a process for the preparation of chlorides of chlorinated carboxylic acids of formula in which R2 denotes the radical (CH2)n, n being an integer from 2 to 4, or the radical -CH2-C(C6H5)2- and R1 denotes a hydrogen atom or an alkyl radical containing from 1 to 4 carbon atoms, which consists in reacting the lactones of formula in which R1 and R2 have the above meanings, with phosgene at a temperature of 90 DEG to 180 DEG C., while employing as catalysts trisubstituted phosphine oxides or sulphides. The process according to the invention makes it possible to obtain chlorides of chlorinated carboxylic acids of high purity which exhibit an excellent stability to light and to heat and which are very useful as synthesis intermediates.
专利号:CN-110790724-B 优先权日:2019-09-20 标题:A kind of selective carbonic anhydrase inhibitor and its synthesis method and application
专利号:CN-110790724-A 优先权日:2019-09-20 标题 :A kind of selective carbonic anhydrase inhibitor and its synthesis method and application
参考标题:1,3-Diketones From Acid Chlorides And Ketones: A Rapid And General One-Pot Synthesis Of Pyrazoles 作者:Stephen T. Heller,Swaminathan R. Natarajan |发布日期:2006.6.1 摘要:[reaction: See Text] 1,3-Diketones Were Synthesized Directly From Ketones And Acid Chlorides And Were Then Converted In Situ Into Pyrazoles By The Addition Of Hydrazine. This Method Is Extremely Fast, General, And Chemoselective, Allowing For The Synthesis Of Previously Inaccessible Pyrazoles And Synthetically Demanding Pyrazole-Containing Fused Rings.
合成参考文献
摘要:Wang, C.; Yang, F., Science of Synthesis: Special Topics, (2022) 1, 448.