专利号:EP-1431274-B1 优先权日:2002-12-18 标题 :Synthesis of mono-N-substituted functionalized anilines 发明人:SELVA MAURIZIO; TUNDO PIETRO 权利人:CONSORZIO INTERUNIVERSITARIO N 摘要:The present invention relates to a process for direct and selective synthesis of mono-N-substituted functionalized anilines by using alkylating agents selected from the class of organic carbonates, preferably of the dialkyl, dibenzyl and diallyl types, in the presence of suitable catalysts that are chemically related to the class of aluminosilicates.
专利号:US-11518780-B2 优先权日:2019-07-31 标 题:Sensitive oligonucleotide synthesis using sulfur-based functions as protecting groups and linkers 发明人:FANG SHIYUE 权利人:FANG SHIYUE 摘要:Embodiments for the synthesis of sensitive oligonucleotides as well as insensitive oligonucleotides are provided. Sulfur-based groups are used for the protection of exo-amino groups of nucleobases, phosphate groups and 2′—OH groups, and as cleavable linker for linking oligonucleotides to a support. Oligonucleotide syntheses are achieved under typical conditions using phosphoramidite chemistry with important modifications. To prevent replacing sulfur-based protecting groups by acyl groups via cap-exchange, special capping agents are used. To retain hydrophobic tag to assist RP HPLC purification, special phosphoramidites are used in the last synthetic cycle. With the sulfur-based groups for protection and linking, oligonucleotide deprotection and cleavage are achieved via oxidation followed by beta-elimination under mild conditions. Therefore, besides for insensitive oligonucleotide synthesis, the embodiments of the invention are capable for the synthesis of oligonucleotide analogs containing sensitive functional groups that cannot survive the harsh conditions used in prior art oligonucleotide synthesis technologies.
专利号:US-6723843-B2 优先权日:1996-08-26 标题:Oligosaccharide synthesis 发明人:TOTH ISTVAN; DEKANY GYULA; KELLAM BARRY 权利人:ALCHEMIA PTY LTD 摘要:The invention provides a system for solid-phase synthesis of oligosaccharides, based on the discovery that a 2-substituted-1,3-dioxocycloalkyl linker group of general formula (I) can be used to couple saccharide groups of both the O-glycoside and N-glycoside type to a polymer support. The invention provides reagents, reagent kits and methods for solid-phase oligosaccharide synthesis.
专利号:US-2024400608-A1 优先权日:2021-09-03 标题:Synthesis of bicycle toxin conjugates, and intermediates thereof 发明人:WITTY DAVID; LIMB DARREN; MIN BYOUNG JOON; HE LIWEN; SANDERS WILLIAM J; NNANABU ERNEST OBINNA 权利人:BRICYCLETX LTD 摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.
专利号:US-7056348-B2 优先权日:2001-04-19 标题:5-aryl-1,3,3-trimethyl-2-methylene-indoline derivatives and salts thereof, methods for the production and use of said compounds for the temporary coloration of fibers 发明人:SAUTER GUIDO; BRAUN HANS-JUERGEN; REICHLIN NADIA 权利人:WELLA AG 摘要:A method for the synthesis of 5-aryl-1,3,3,-trimethyl-2-methylene-indoline derivatives of Formula (I) or its salts of Formula (Ia) wherein 1 mole of a 5-aryl-2,3,3-trimethyl-3H-indole derivative of Formula (VII) is reacted for 1 to 44 hours at a temperature of 20° to 180° C. in an apolar, aprotic or polar, protic or polar aprotic solvent with 1 to 50 moles of a compound of Formula R1-A; new compounds of Formulas (I)/(Ia) and (V), obtainable by this method as well as an agent containing at least one compound of Formula (I)/(Ia) and a carbonyl/imine compound for dyeing keratinic fibers and a method for temporarily dyeing keratin fibers, for which the keratin fiber is dyed with the aforementioned agent and the dyeing, so obtained, is removed again at any later time by a sulfite preparation.
专利号:US-8895747-B2 优先权日:2009-07-27 标 题 :Method and substances for preparation of N-substituted pyridinium compounds 发明人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL 权利人:HEINDL DIETER; MAERZ HERIBERT; SCHMIDT AXEL; ROCHE DIAGNOSTICS OPERATIONS 摘要:Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
[参考文献]: Franciscus M H De Groot, Et Al. Design, Synthesis, And Biological Evaluation Of A Dual Tumor-Specific Motive Containing Integrin-Targeted Plasmin-Cleavable Doxorubicin Prodrug. Mol Cancer Ther. 2002 Sep;1(11):901-11. [参考文献]: Katarzyna Gorska, Et Al. Dna-Templated Release Of Functional Molecules With An Azide-Reduction-Triggered Immolative Linker. Chem Commun (Camb). 2011 Apr 21;47(15):4364-6.
合成参考文献
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