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:WO-0146142-A1 优先权日:1999-12-20 标题:A process for the regioselective synthesis of 2,2-dialkyl-4-substituted piperidines 发明人:HEATH PERRY CLARK 权利人:LILLY CO ELI; HEATH PERRY CLARK 摘要:The present invention provides a process for preparing a compound of formula (I): wherein R?1 and R2¿ each independently represent C¿1?-C4 alkyl; and X represents an alkyl, alkenyl, cycloalkyl, aryl, substituted aryl, heterocycle, or substituted heterocycle, comprising treating a compound of formula (II): wherein Q represents Cl or Br, with a suitable base followed by addition of a suitable Lewis acid and addition of a compound of formula R?-M+¿ wherein M+ is a suitable cation.
专利号:US-4292249-A 优先权日:1979-02-15 标题:25-Hydroxy-24-oxocholestane derivatives and preparation thereof 发明人:NISHIKAWA OSAMU; ISHIMARU KENJI; TAKESHITA TORU; TSURUTA HIDEKI 权利人:TEIJIN LTD 摘要:This invention relates to novel 25-hydroxy-24-oxocholestane derivatives and a process for preparing them. The novel 25-hydroxy-24-oxocholestane derivatives of this invention can easily be converted to 24,25-dihydroxycholecalciferol or 1 alpha ,24,25-trihydroxycholecalciferol which is known as useful for medicine controlling the calcium metabolism of warm-blooded animals. Moreover, 25-hydroxy-24-oxocholestane derivatives can be converted to novel 25-hydroxy-24-oxocholecalciferol expressed by the following formula and novel 1 alpha ,25-dihydroxy-24-oxocholecalciferol of the formula which are useful for medicine. The new 25-hydroxy-24-oxocholestane derivatives in the present invention are very useful as the intermediates for the synthesis of a variety of active vitamin D3.
专利号:US-7674904-B2 优先权日:2005-05-25 标 题 :Synthesis of R-N-methylnaltrexone
专利号:US-2007099946-A1 优先权日:2005-05-25 标 题:Synthesis of R-N-methylnaltrexone
专利号:US-4035405-A 优先权日:1976-07-09 标题 :Novel synthesis for preparing the hydrochloride salt of selected catecholamine derivatives 发明人:BODOR NICOLAE S; YUAN SUN-SHINE 权利人:INTERX RESEARCH CORP 摘要:Compounds of the formula: ##STR1## wherein R represents a straight or branched C 1 -C 5 alkyl group; and R 1 in each occurrence represents an acyl member which is alkanoyl having 1-22 carbon atoms, alkenoyl having one or two double bonds and having 4-22 carbon atoms, ##STR2## having a total of 4-10 carbon atoms of which 3-7 are ring carbon atoms in cycloalkyl and wherein n is zero, one, or two, phenoxyacetyl, naphthalenecarbonyl, pyridinecarbonyl, ##STR3## wherein n is zero, one or two and phenyl is unsubstituted or is substituted by 1-3 alkyl having 1-4 carbon atoms, alkoxy having 1-4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2-8 carbon atoms, or alkanoylamino having 1-6 carbon atoms groups; are prepared in substantial purity and yield, using as the chloride ion donor, cesium chloride (CsCl). n The compounds prepared by the process claimed herein exhibit sympathomimetic activity and are thus useful in eliciting sympathomimetic responses in warm-blooded animals, e.g., reduction in intraocular pressure, miosis, mydriasis, bronchodilation, etc.
[参考文献]: Mingzhang Gao, Et Al. Synthesis Of Carbon-11 Labeled 1-(3,4-Dimethoxybenzyl)-2,2-Dimethyl-1,2,3,4-Tetrahydroisoquinolinium Derivatives As New Potential Pet Skca Channel Imaging Agents. Appl Radiat Isot. 2008 Feb;66(2):194-202.
合成参考文献
摘要:Goldfuss, B., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 1, 429. 参考文献:10.1007/bf00245162 摘要:Kataoka M, Shimizu S, Yamada H. Distribution and immunological characterization of microbial aldehyde reductases. Arch Microbiol. 1992;157(3):279–83. doi: 10.1007/bf00245162.