专利号:US-7102023-B2 优先权日:1999-11-24 标 题:Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 发明人:BUCHWALD STEPHEN L; PLANTE OBADIAH J; SEEBERGER PETER H 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
专利号:US-6235871-B1 优先权日:1997-12-03 标题:Synthesis of oligoarylamines, and uses and reagents related thereto 发明人:SINGER ROBERT A; SADIGHI JOSEPH P; BUCHWALD STEPHEN L; MACKEWITZ THOMAS 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The transition metal-catalyzed amination of aryl halides, in conjunction with an orthogonal protective group scheme, forms the basis of two routes to oligoaniline precursors. The oligoaniline precursors are soluble in a variety of common organic solvents, and are easily converted to the deprotected oligoanilines. The method allows the preparation of oligoanilines of even or odd chain lengths, and the incorporation of a variety of functional groups into the oligomers. Polyanilines of low polydispersity can also be prepared by this method.
专利号:US-2024101516-A1 优先权日:2021-01-20 标 题:Synthesis of polyfluorinated aryl and heteroaryl carboxamides 发明人:KADUSKAR RAHUL; BORATE KAILASKUMAR; ADHAV SUYOG; THIRUNAVUKKARASU SARAVANAN; SHINDE HARISH; GOETZ ROLAND 权利人:BASF SE 摘要:The presently claimed invention relates to a process for the preparation of mono-, di-, tri-, fluoro arylamide or hetroarylamide.
专利号:US-2014011992-A1 优先权日:2012-12-20 标 题:Synthesis of abiraterone and related compounds 发明人:PEREZ ENCABO ALFONSO; TURIEL HERNANDEZ JOSE ANGEL; GALLO NIETO FRANCISCO JAVIER; LORENTE BONDE-LARSEN ANTONIO; SANDOVAL RODRIGUEZ CELSO MIGUEL 权利人:CRYSTAL PHARMA SAU 摘要:The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C—C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.
专利号:US-10457640-B2 优先权日:2016-10-19 标 题:Synthesis of inhibitors of EZH2 发明人:VASWANI RISHI G; HEWITT MICHAEL CHARLES 权利人:CONSTELLATION PHARMACEUTICALS INC 摘要:Provided herein are synthetic methods for the preparation of EZH2 inhibitors.
专利号:US-6465693-B2 优先权日:1998-02-26 标 题 :Metal-catalyzed arylations of hydrazines, hydrazones, and related substrates 发明人:BUCHWALD STEPHEN L; WAGAW SEBLE; GEIS O 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.