专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-9597327-B2 优先权日:2005-05-25 标 题:Synthesis of (R)-N-methylnaltrexone 发明人:DOSHAN HAROLD D; PEREZ JULIO 权利人:PROGENICS PHARM INC 摘要:This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
专利号:US-10266503-B1 优先权日:2016-05-24 标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins 发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN 权利人:UNIV ILLINOIS 摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.
专利号:US-8148527-B1 优先权日:2011-01-18 标 题:Resolution of 1-(4-methoxybenzyl)-octahydro-isoquinoline 发明人:DIVI MURALI KRISHNA PRASAD; PENDYALA SRINIVAS RAO; RAMANA LAVU VENKATA 权利人:DIVI MURALI KRISHNA PRASAD; PENDYALA SRINIVAS RAO; RAMANA LAVU VENKATA; DIVIS LAB LTD 摘要:The resolution of racemic 1-(4-methoxybenzyl)-octahydro-isoquinoline, a key intermediate in the synthesis of the antitussive agent dextromethorphan, is reported using (R)-2-(6-methoxy-2-naphthyl) propionic acid in good yields. The resolving agent and the undesired isomer of the octahydro-isoquinoline have been recovered in good yield.
专利号:US-2021062179-A1 优先权日:2015-02-26 标题 :Microsomal bioreactor for synthesis of drug metabolites 发明人:KRISHNAN SADAGOPAN; WALGAMA CHARUKSHA THAMEERA; NERIMETLA RAJASEKHARA REDDY 权利人:UNIV OKLAHOMA STATE 摘要:Reusable microsomal biocatalytic systems (bioreactors) constructed on carbon nanostructure modified electrodes are provided. The bioreactors comprise stable, biologically active immobilized enzymes such as human cytochromes P 450 (CYPs) and their redox partner proteins, e.g. CYP-NADPH (reduced nicotinamide adenine dinucleotide phosphate) reductases (CPR), on the carbon nanostructure surface. The immobilized enzymes may be present in liver microsomes, such as human liver microsomes (HLM) or as bactosomes, S9 fractions, etc. The bioreactors are used, for example, for synthesizing metabolites of interest from compounds such as drugs that are catabolized by the enzymes.
专利号:BR-PI0710538-A2 优先权日:2006-04-20 标 题:process for the synthesis of a substantially pure stereoisomer, compounds, pharmaceutical composition comprising a compound, process for the synthesis of a compound and use thereof.