专利号:US-2023183223-A1 优先权日:2020-05-14 标题:Process for the synthesis of n-butyloxycarbonyl-3-(4-imidazol-1- ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide 发明人:CERNAKS DMITRIJS; DEGE ELIZA 权利人:VICORE PHARMA AB 摘要:There is provided a new process for the synthesis of compounds of formula I, which are useful as angiotensin (Ang II) type 2 receptor agonists: by reacting a compound of formula II, with an excess of a compound of formula III, wherein W, Z and X have meanings given in the description; followed by reaction of the intermediate so formed with a suitable source of the counter-ion, W.
专利号:US-6919382-B2 优先权日:2000-08-31 标 题 :Preparation and uses of conjugated solid supports for boronic acids 发明人:HALL DENNIS G 权利人:UNIV ALBERTA 摘要:The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.
专利号:CN-115836066-A 优先权日:2020-05-14 标 题:Synthesis of N-butoxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-isobutylthiophene-2-sulfonamide
专利号:EP-4149942-A1 优先权日:2020-05-14 标题 :Process for the synthesis of n-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide
专利号:WO-2021229244-A1 优先权日:2020-05-14 标 题 :Process for the synthesis of n-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide
专利号:CA-3178112-A1 优先权日:2020-05-14 标 题:Process for the synthesis of n-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide
[参考文献]: Chongyi Liu, Et Al. Clustering Small Dendrimers Into Nanoaggregates For Efficient Dna And Sirna Delivery With Minimal Toxicity. Adv Healthc Mater. 2016 Mar 9;5(5):584-92.
合成参考文献
摘要:Harsanyi, A.; Sandford, G., Science of Synthesis Knowledge Updates, (2015) 1, 165. 参考文献:10.1021/jm200310q 摘要:Albers HM, Hendrickx LJ, van Tol RJ, Hausmann J, Perrakis A, Ovaa H. Structure-based design of novel boronic acid-based inhibitors of autotaxin. J Med Chem. 2011 Jul 14;54(13):4619–26.