专利号:US-4749806-A 优先权日:1984-12-28 标题:Process for the synthesis of isocyanates and of isocyanate derivatives 发明人:TKATCHENKO IGOR; JAOUHARI RABIH; BONNET MICHEL; DAWKINS GORDON; LECOLIER SERGE 权利人:POUDRES & EXPLOSIFS STE NALE 摘要:The present invention relates to a process for the synthesis of isocyanates and of isocyanate derivatives. Isocyanates are obtained by reacting an organic halide with a metal cyanate in an organic medium in the presence of a catalyst consisting of a complex of nickel with at least one organic ligand, in which complex the nickel is in the zero oxidation state. A carbamate or a urea, respectively, are obtained by a subsequent reaction with a hydroxy compound or a primary or secondary amine. Isocyanates and their derivatives are used especially either as refined synthesis agents for the production of pesticides and medications, or as monomers or comonomers for the preparation of many macromolecular compounds.
专利号:WO-2024218783-A1 优先权日:2023-04-17 标题 :Green chemistry approach for synthesis of mavacamten and its intermediate using novel methodology 发明人:CHEEPIRISHETTI SHANKAR; CHEEPIRISHETTI ASHRIT; KOMARRAJ SNEHITHA; KAUSHAL KISHORE; BORREDDY SIVA PRASAD REDDY; BASANTHI DEVI; SHAIK SAYYAD SHAMSHUDDIN; KUMAR MUKES 权利人:DASHA PHARMACEUTICALS PRIVATE LTD 摘要:The present invention discloses a green chemistry approach for synthesis of Mavacamten (Compound of formula I). The present invention also discloses a novel process for preparation of an intermediate 1-isopropylpyrimidine-2,4,6(1H,3H,5H)-trione (Compound of formula VII) and further preparation of Mavacamten using this intermediate, following novel methodology.
专利号:US-12281398-B2 优先权日:2022-02-07 标题:Microfluidic process for the general electrochemical synthesis of geminal dipseudohalide or halide-pseudohalide compounds 发明人:SCHROER THORSTEN G; LECROY GREGORY E; AGUILA MIGUEL; RODRIGUEZ MAYRA P; DOWNARD TYLER J; MACLEOD BRIANNA L 权利人:US GOV AIR FORCE; US AIR FORCE 摘要:A process for the microfluidic electrochemical synthesis of geminal dipseudohalide or halide-pseudohalide compounds comprising the steps ofpumping a solution comprising a compound of Formula Iinto a microfluidic electrochemical reactor in the presence of a base, one of a halide or pseudohalide salt (MY), and a mediator;applying an electrical current through the microfluidic electrochemical reactor; andperforming oxidative addition to create a geminal dipseudohalide or halide-pseudohalide compound of the general Formula II
专利号:US-12234200-B2 优先权日:2019-04-16 标 题:Synthetic methods of preparing esketamine 发明人:CHEN CHENG YI 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to methods for the asymmetric synthesis of esketamine. The present invention is further directed to key intermediates in the asymmetric esketamine synthesis. In one embodiment, the invention is an asymmetric synthesis of esketamine comprising the conversion of (S)-2′-chloro-2-methoxy-3,4,5,6-5 tetrahydro-[1, 1′-biphenyl]-3-yl carbamate to (S)-2′-chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1′-biphenyl.
专利号:US-6080860-A 优先权日:1992-08-31 标 题:Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor 发明人:KARIMIAN KHASHAYAR; MURTHY KESHAVA; HALL DARREN 权利人:BRANTFORD CHEMICALSS INC 摘要:Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.
专利号:WO-0168615-A1 优先权日:2000-03-13 标题 :Quinazoline synthesis 发明人:DENER JEFFREY MARK; LEASE TIMOTHY G; NOVACK AARON ROBERT 权利人:CHEMRX ADVANCED TECHNOLOGIES I; DENER JEFFREY MARK; LEASE TIMOTHY G; NOVACK AARON ROBERT 摘要:The present invention relates to a method for making a compound of Formulas I, II and III. The method of the present invention also enables parallel and simultaneous synthesis of a plurality of compounds represented by Formulas I, II and III.
参考文献:10.1007/s00726-011-0975-2 摘要:Danger G, Charlot S, Boiteau L, Pascal R. Activation of carboxyl group with cyanate: peptide bond formation from dicarboxylic acids. Amino Acids. 2012 Jun;42(6):2331–41. doi: 10.1007/s00726-011-0975-2.