丁二酸单甲酯 反应生成3-溴丙酸甲酯 参考文献:Thallium In Organic Synthesis. Vi. Synthesis Of Primary Aliphatic Bromides 标题:Thallium In Organic Synthesis. Vi. Synthesis Of Primary Aliphatic Bromides 摘要: Doi:10.1021/jo01256A104
专利号:US-8178712-B2 优先权日:2006-06-23 标 题:Process for the synthesis of Ibandronate sodium 发明人:RAO DHARAMARAJ RAMCHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI GANPATI 权利人:RAO DHARAMARAJ RAMCHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI GANPATI; CIPLA LTD 摘要:The present invention relates to an improved process for the synthesis of Ibandronate sodium of formula (I). The present invention also provides novel processes for the synthesis of 3-[N-(methylpentyl)amino]propionic acid (III).
专利号:US-9388147-B2 优先权日:2009-11-13 标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN 权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-9254327-B2 优先权日:2010-05-10 标 题 :Methods and compositions for delivery of active agents 发明人:MANOHARAN MUTHIAH; RAJEEV KALLANTHOTTATHIL G 权利人:MANOHARAN MUTHIAH; RAJEEV KALLANTHOTTATHIL G; ALNYLAM PHARMACEUTICALS INC 摘要:A lipid particle can include a cationic lipid. Synthesis of the cationic lipid can include a ylide-based reaction, such as a Wittig reaction or sulfur ylide reaction. In some cases, the synthesis can also include a Michael addition or a related addition reaction.
专利号:US-4111933-A 优先权日:1976-04-30 标题:Protection of functional groups during reaction and their subsequent restoration 发明人:ECKERT HEINER; UGI IVAR; KABBE HANS-JOACHIM 权利人:BAYER AG 摘要:In the process for preparing an organic compound of the formula n n A' -- X n n in which n X is an amino group, a hydroxyl group or a carboxyl group, and n A' is the remainder of the molecule, from an organic compound of the formula n n A -- X n n in which n A is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formula n n A -- Z -- COOR n n in which n Z is --NH--, --O-- or a direct C--C bond, and n R is a radical of the formula ##STR1## IN WHICH Y is a direct C--C single bond, the --CHâ•?CH-- group or an arylene group, n R 1 to R 4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, or n R 1 + r 2 and R 3 + R 4 each independently completes a 5- or 6-membered carbocyclic ring, or n R 1 and R 3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen, n Thereby to protect X, then converting A -- Z -- COOR into a compound of the formula n n A' -- Z -- COOR n n and then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporis.
专利号:US-9605019-B2 优先权日:2011-07-19 标 题:Methods for the synthesis of functionalized nucleic acids 发明人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL 权利人:VERDINE GREGORY L; MEENA; IWAMOTO NAOKI; BUTLER DAVID CHARLES DONNELL; WAVE LIFE SCIENCES LTD 摘要:The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.
专利号:US-6593347-B2 优先权日:1998-10-30 标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
摘要:Chciuk, T. V.; Flowers, R. A.; Flowers, R. A., Science of Synthesis Knowledge Updates, (2016) 2, 197. 摘要:Garve, L. K. B.; Werz, D. B., Science of Synthesis: Metal-Catalyzed Cyclization Reactions, (2016) 2, 88. 摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 1985. Acute oral toxicity and repellency of 933 chemicals to house and deer mice. Archives of Environmental Contamination and Toxicology 14:111-129. 参考文献:10.1107/s1600536810020234 摘要:Haridharan N, Ramkumar V, Dhamodharan R. 2-Oxo-4-trifluoro-meth-yl-2H-chromen-7-yl 2-bromo-2-methyl-propano-ate. Acta Crystallogr Sect E Struct Rep Online. 2010 Jun 09;66(Pt 7):o1606.