专利号:US-6274383-B1 优先权日:1997-12-15 标题:Methods for synthesizing libraries of dihydro-quinazolinones 发明人:GAO YUN 权利人:SEPRACOR INC 摘要:Synthetic methods for solution and solid-phase synthesis of combinatorial libraries of dihydro-quinazolinones, including synthesis of 2,3-dihydro-3-alkoxy-4(1H)-quinazolinones or 2,3-dihydro-3-hydroxy-4(1H)-quinazolinones via the Lewis-acid catalyzed reaction of an appropriate 2-aminobenzamide with an aldehyde at ambient temperature performed on a solid support or in solution.
专利号:US-5786448-A 优先权日:1996-11-07 标题:Combinatorial libraries of cyclic urea and cyclic thiourea derivatives and compounds therein 发明人:NEFZI ADEL; OSTRESH JOHN M; HOUGHTEN RICHARD 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of cyclic urea and cyclic thiourea compounds. The present invention further provides the compounds made by the combinatorial synthesis.
专利号:US-6156494-A 优先权日:1997-10-28 标题 :Serially directed combinatorial synthesis on fiber optic arrays 发明人:ADAMS CHRISTOPHER; BOLES T CHRISTIAN; SRIDHAR COIMBATORE NAGARAJA 权利人:MOSAIC TECHNOLOGIES 摘要:A method has been developed which utilizes functionalized optical fibers as a solid support for the assembly of combinatorial libraries of compounds. The optical fibers are used to direct light, heat or a combination thereof to the compounds tethered to the fibers surface. Utilizing the method of the instant invention reactions occurring by both photochemically and thermally allowed pathways are accessible. In a preferred embodiment of the invention, the optical fibers are used to screen the array by fluorescence spectroscopy of labeled target molecules which bind to the immobilized library compounds.
专利号:US-2024300982-A1 优先权日:2023-03-03 标题 :Reactive secondary boranes and methods for synthesis thereof 发明人:Martin Caleb; AKRAM MANJUR 权利人:UNIV BAYLOR 摘要:A secondary borane featuring two ortho-carborane substituents [HBoCb2, oCb=ortho-carborane] is useful as a powerful hydroboration reagent. The Lewis superacid, bis(1-methyl-ortho-carboranyl)borane, is rapidly accessed in two steps. It is a very effective hydroboration reagent capable of the hydroboration of alkenes, alkynes, cyclopropanes, and allenes. The large steric profile prevents double hydroboration of alkynes and promotes regioselectivity in allenes. The compound is a Lewis superacidic secondary borane and effective neutral hydroboration reagent.
专利号:US-6809202-B2 优先权日:1996-11-07 标 题 :Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof 发明人:NEFZI ADEL; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl gorup and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
专利号:US-10889574-B2 优先权日:2016-06-17 标 题 :Method for producing diphenylmethane derivative 发明人:YOON HEE-KYOON; PARK SE-HWAN; YOON JI-SUNG; CHOI SOONGYU; SEO HEE JEONG; PARK EUN-JUNG; KONG YOUNGGYU; SONG KWANG-SEOP; KIM MIN JU; PARK SO OK 权利人:DAE WOONG PHARMA; GREEN CROSS CORP 摘要:The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which each major group is separately synthesized and then coupled. As such, in comparison to a linear synthesis method disclosed in existing documents, the synthesis pathway is compact and yield can be increased, and risk factors inherent in the linear synthesis pathway can be reduced. Furthermore, the crystal form of the compound produced according to the method has superb physicochemical characteristics, and thus can be effectively utilized in fields such as pharmaceutical manufacturing.