专利号:US-11370736-B2 优先权日:2019-04-01 标 题:Synthesis of fluoro hemiacetals via transition metal-catalyzed fluoro ester and carboxamide hydrogenation 发明人:DUB PAVEL A; BATRICE RAMI J; GORDON JOHN C 权利人:TRIAD NAT SECURITY LLC 摘要:This application is directed to use of transition metal-ligand complexes to hydrogenate fluorinated esters and carboxamides into fluorinated hemiacetals. Methods for synthesis of certain ligands are also provided.
专利号:US-5399721-A 优先权日:1990-01-12 标题:Synthesis of optically pure 4-aryl-2-hydroxytetronic acids 发明人:HOPPER ALLEN T; WITIAK DONALD T 权利人:UNIV OHIO STATE RES FOUND 摘要:The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. the invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.
专利号:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
专利号:WO-9529150-A1 优先权日:1994-04-21 标 题 :Synthesis of prototypes for renin inhibitors 发明人:HANESSIAN STEPHEN 权利人:CIBA GEIGY AG; HANESSIAN STEPHEN 摘要:Prototype renin inhibitors having general structure (I), where n is 0-3 inclusive, A are either both hydrogen atoms or together are a single carbon-nitrogen bond, R1 is hydrogen, or hydrocarbylcarboxy wherein the hydrocarbyl entity is selected from the group consisting of alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 10 carbon atoms, R2 and R3 or independently alkyl of 1 to 4 carbon atoms, R4 is alkyl of 1 to 6 carbon atoms or a substituent of aliphatic character such as, for example, butyl, 2-morpholinoethyl or 2-carbamoyl-2-methyl-propyl, R5 is selected from aromatics, substitued aromatics and heteroaromatics, substituted or unsubstituted cycloalkyls, cycloalkenes having 3 to 8 carbon atoms, with substituents selected from alkyl, alkoxy of 3 to 10 carbon atoms and alkoxy derivatives such as 3-methoxy-propyloxy, primary and secondary amides, alkyl derivatives, are prepared by novel multistep synthesis. Such compounds are valuable intermediates for the manufacture of pharmaceutical such as Renin inhibitors and HIV-protease inhibitors.
专利号:US-4978744-A 优先权日:1989-01-27 标题:Synthesis of dolastatin 10 发明人:PETTIT GEORGE R; SINGH SHEO B 权利人:UNIV ARIZONA 摘要:A complicated but extremely important scheme of synthesis has been developed for synthesizing, dolaisoleuine, dolaproine, dolaphenine and dolavaline from readily available starting materials such as Z-(S,S)isoleucine, S-phenylalaline, S-phenylalaninol, S-prolinol, S-mandelate, and S-valine. The requisite amino acids have been combined using several peptide coupling procedures to create pharmaceutically pure dolastatin 10.
专利号:US-6469193-B1 优先权日:1999-02-26 标 题 :Efficient synthesis of alkyl carbonates 发明人:JUNG KYUNG WOON 权利人:UNIV SOUTH FLORIDA 摘要:Efficient synthetic methods towards mixed aliphatic carbonates through the three component couplings of aliphatic alcohols, alkyl halides and carbon dioxide in the presence of cesium carbonate and tetrabutylammonium iode (TBAI). Due to their enhanced nucleophilicities, cesium alkoxides are smoothly incorporated into CO 2 , allowing for mild reaction conditions such as ambient temperatures and short reaction durations. Various primary and secondary substrates are compatible under the standard conditions, offering high yields, while chiral templates such as α-hydroxy carbonyls are resistant to racemization.
摘要:Zaidlewicz, M.; Pakulski, M. M., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 85. 摘要:Wu, X.; Xiao, J., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 282. 摘要:Riva, R.; Banfi, L.; Basso, A., Science of Synthesis: Multicomponent Reactions, (2013) 1, 398.