专利号:US-10829792-B2 优先权日:2017-03-21 标 题 :Biocatalytic synthesis of strained carbocycles 发明人:CHEN KAI; HUANG XIONGYI; KAN S B JENNIFER 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein are methods for producing products containing strained carbocycles, such as cyclopropene moieties and/or bicyclobutane moieties. The methods include combining an alkyne and a carbene precursor in the presence of a heme protein, e.g., a cytochrome P450, under conditions sufficient to form the strained carbocycle. Reaction mixtures for producing strained carbocycles are also described, as well as whole-cell catalysts comprising heme proteins and variants thereof for forming cyclopropenes, bicyclobutanes, and related products.
专利号:WO-2018217538-A1 优先权日:2017-05-23 标题 :Synthesis of substituted acridines 发明人:FORT ERIC H; JAYE JOSEPH A; MCCORMICK GRANT M; BERGER KRISTEN E 权利人:UNIV OF ST THOMAS 摘要:Disclosed is a method of making substituted acridines. The method includes the step of reacting a bis(halophenyl) amine with an alkyne for a time and at a temperature to yield a substituted acridine.
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-8835658-B2 优先权日:2012-12-28 标 题:Asymmetric synthesis of norcantharidin analougus by alkynylation of oxabenzonorbornadienes and their anticancer activities 发明人:CHAN ALBERT SUN-CHI; FAN BAOMIN; WANG JUN; LIN CHENGYUAN; HUANG CHAO; YANG QINGJING; XU JIANBIN; BIAN ZHAOXIANG; LU AIPING; HU JUN 权利人:UNIV HONG KONG BAPTIST; UNIV YUNNAN NATIONALITIES 摘要:The present invention relates to a type of norcantharidin analogues and a method to synthesis such norcantharidin analogues by transition metal-catalyzed alkynylation of 7-oxabenzonorbornadienes. The present invention also relates to the use of such norcantharidin analogues in manufacture of a medicament for the treatment of cancer tumors.
专利号:US-8242273-B2 优先权日:2005-07-28 标 题:Synthesis of 4/5-pyrimidinylimidazoles via sequential functionalization of 2,4-dichloropyrimidine 发明人:DENG XIAOHU; MANI NEELAKANDHA 权利人:DENG XIAOHU; MANI NEELAKANDHA; JANSSEN PHARMACEUTICA NV 摘要:This invention relates to methods of making pyrimidinyl-substituted imidazole compounds by sequential substitution of the 4- and 2-chloro groups of 2,4-dichloropyrimidine, nucleophilic substitution to form pyrimidinylalkyne derivatives, oxidation to the corresponding 1,2-diketones, and cyclocondensation reactions.
专利号:US-11033889-B2 优先权日:2018-10-23 标 题:Palladium acyclic diaminocarbene complexes as precatalysts for Hiyama coupling and the tandem one-pot fluoride free Hiyama coupling/cyclization for the synthesis of biologically relevant 发明人:SINGH CHANDAN; GHOSH PRASENJIT 权利人:INDIAN INST TECHNOLOGY BOMBAY 摘要:The present invention provides Acyclic diaminocarbene complex of formula (I):Wherein,M is palladium;X is monoanionic ligand selected from Cl, Br or I;Where R1 is different from R2;R1 is selected from the group consisting of alkyl or aryl, each of which have 4 to 20 carbon atoms, and may optionally contain one or more heteroatoms;R2 is selected from the group consisting of alkyl, or aryl each of which have 4 to 20 carbon atoms, and may optionally contain one or more heteroatoms. The said palladium diamino carbine complex of the present invention are particularly useful as catalyst from Hiyama cross-coupling reaction.
[参考文献]: Johan R Johansson, Et Al. Sequential One-Pot Ruthenium-Catalyzed Azide-Alkyne Cycloaddition From Primary Alkyl Halides And Sodium Azide. J Org Chem. 2011 Apr 1;76(7):2355-9.
合成参考文献
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