专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-4460793-A 优先权日:1980-12-30 标 题:Preparation of monochloromethyl ketones 发明人:JAUTELAT MANFRED; ARLT DIETER; JAEGER GERHARD 权利人:BAYER AG 摘要:A process for the production of a monochloromethyl ketone of the formula in which R1, R2 and R3 each independently is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkinyl or aryl radical, or R1 and R2 together with the carbon atom to which they are attached form an optionally substituted carbocyclic ring, comprising reacting a 1,1-dichloroalkene of the formula with a phenolate of the formula in which R4 each independently is a halogen atom, a nitro group, or an optionally substituted alkyl, alkoxy or aryl radical, n is 0, 1, 2 or 3, and M is one equivalent of an alkali metal ion or alkaline earth metal ion, thereby to obtain a phenyl ether intermediate, and then subjecting the phenyl ether intermediate to an acid hydrolysis. The products are useful as intermediates in the synthesis of fungicides.
专利号:US-10329268-B2 优先权日:2013-09-13 标 题 :Processes for preparing medicaments for the treatment of cardiovascular diseases and intermediates for use therein 发明人:RUSSO DOMENICO; WAHNON JORGE; MATON WILLIAM; WEBER BEAT T; JERONIMO PAULA; SOUSA LUISA; BARROCAS PEDRO; PIRES RITA; LIMA RICARDO; VASCONCELOS TEOFILO 权利人:BIAL PORTELA & CA SA 摘要:The present invention provides a compound of formula N wherein: X is CH 2 , oxygen or sulphur; R 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group, wherein N is in the form of the individual R- and S-enantiomer or a mixture of the (R)- and (S)-enantiomer. The present invention also provides a compound of formula MA. The present invention also provides processes for preparing the above compounds, and processes involving their use. The compounds are particularly useful as intermediates in the synthesis of peripherally-selective inhibitors of dopamine-β-hydroxylase.
专利号:US-5567830-A 优先权日:1994-02-14 标题 :Process for synthesis of acetylenic carbinols 发明人:UPASANI RAVINDRA B 权利人:COCENSYS INC 摘要:A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.
专利号:US-5442093-A 优先权日:1994-05-09 标题:Process for preparing intermediates for the synthesis of antifungal agents 发明人:SUDHAKAR ANANTHA 权利人:SCHERING CORP 摘要:Disclosed is a process for preparing compounds of the formula I ##STR1## wherein R is C 1 -C 6 alkyl, comprising heating a mixture of a difluorobenzene derivative, allene, a dialkyl malonate of the formula CH 2 (CO 2 R) 2 , wherein R is C 1 -C 6 alkyl, and a base, in a polar organic solvent in the presence of a catalyst.
专利号:WO-2013131872-A1 优先权日:2012-03-05 标 题 :Imaging neural activity 发明人:BETTS HELEN MAY; DESMOND ANTONIA; ROBINS EDWARD GEORGE 权利人:GE HEALTHCARE LTD; UCL SCHOOL OF PHARMACY 摘要:The present invention provides a novel radiofluorinated compound for imaging voltage-gated sodium channels (VGSCs) that is more straightforward to synthesise than the known radiofluorinated phenoxyphenyl pyrazole carboxylic acid compounds. The compound of the present invention demonstrates specific uptake and retention in key tissues as well as good in vivo stability. Also provided by the present invention is a radiopharmaceutical composition comprising the radiofluorinated compound of the invention, precursor compounds and methods for the synthesis of said radiofluorinated compound, and methods for using said radiofluorinated compound.
[参考文献]: W C Sun, Et Al. Synthesis Of Novel Fluorinated Coumarins: Excellent Uv-Light Excitable Fluorescent Dyes. Bioorg Med Chem Lett. 1998 Nov 17;8(22):3107-10.
合成参考文献
参考文献:10.1107/s1600536810040080 摘要:Kubono K, Tsuno Y, Tani K, Yokoi K. Aqua-{4,4',6,6'-tetra-fluoro-2,2'-[(piperazine-1,4-di-yl)dimethyl-ene]diphenolato}copper(II). Acta Crystallogr Sect E Struct Rep Online. 2010 Oct 13;66(Pt 11):m1397–8.