专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-3635999-A 优先权日:1969-03-25 标 题 :Synthesis of oxazoles 发明人:TRAMIER BERNARD; BONZOM ALBERT 权利人:AQUITAINE PETROLE 摘要:WHERE R2 IS ALKYL OF 1 TO 6 CARBON ATOMS, PHENYL OR HYDROXYPHENYL, R4 IS METHYL AND R5 IS HYDROGEN. A PROCESS OF PREPARING OXAZOLES IS DISCLOSED COMPRISING CONDENSING AN ACETYLENIC COMPOUND HAVING AN ELECTRONEGATIVE GROUP ON THE CARBON ATOM IN THE X-POSITION RELATIVE TO THE TRIPLE BOND WITH AN AMMONIUM SALT OF AN ORGANIC ACID OR AN AMIDE. 2-R2,4-R4,5-R5-OXAZOLE NEW OXAZOLES ARE PREPARED HAVING THE FORMULA
专利号:US-8269047-B2 优先权日:2009-07-23 标题 :Synthesis of alpha-halo enones and enals 发明人:ZHANG LIMING; YE LONGWU 权利人:ZHANG LIMING; YE LONGWU; UNIV NEVADA 摘要:A method for preparing an α-halo enal or enone from an unprotected propargyl alcohol and an electrophilic halogen source catalyzed by the combination of a gold catalyst complex and a metal co-catalyst complex is disclosed. The method can be further enhanced by addition of an additive that facilitates suppression of a des-halo derivative.
专利号:US-5637757-A 优先权日:1995-04-11 标 题 :One-pot synthesis of ring-brominated benzoate compounds 发明人:HILL JOHN E; FAVSTRITSKY NICOLAI A; MAMUZIC RASTKO I; BHATTACHARYA BHABATOSH 权利人:GREAT LAKES CHEMICAL CORP 摘要:A method of preparing tetrabromobenzoate compounds from tetrabromophthalic anhydride by reacting tetrabromophthalic anhydride with alcohol in the presence of a decarboxylation catalyst. The reaction may be carried out in an excess of alcohol, or with a near stoichiometric amount of alcohol by performing the reaction in an inert solvent.
专利号:US-3676442-A 优先权日:1968-11-22 标 题:Synthesis of pyrazines 发明人:BONZOM ALBERT; TRAMIER BERNARD 权利人:AQUITAINE PETROLE 摘要:Hydrocarbon substituted pyrazines are prepared by the reaction of an ammonium compound having NH4 or NH2 groups with an acetylene compound having an oxygen atom linked to the acetylenic unit, the reaction being conducted in an acid medium, preferably containing formic acid or a formate.
专利号:US-3978100-A 优先权日:1973-04-18 标题:Allenic esters, process for preparation thereof and process for rearrangement thereof 发明人:FUJITA YOSHIJI; OMURA YOSHIAKI; HISHIDA TAKASHI; ITOI KAZUO 权利人:KURARAY CO 摘要:Allenic esters of the formula: ##EQU1## (specific examples of R, R 1 , R 2 , R 3 and R 4 are given) and a process for the preparation thereof which comprises reacting propargyl alcohol derivatives with 2-substituted ortho-acetic acid esters in the presence of an acidic catalyst. These allenic esters are rearranged in the presence of an alkali catalyst to form α, β, γ, δ-unsaturated carboxylic acid esters and are useful as intermediates in the synthesis of various perfumes, medicines, agricultural chemicals and the like.
摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2014) 4, 74. 摘要:Dornan, L. M.; Hughes, N. L.; Muldoon, M. J., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 539.