专利号:US-6579725-B1 优先权日:1999-03-05 标题 :Linkers for synthesis of oligosaccharides on solid supports 发明人:SEEBERGER PETER H; ANDRADE RODRIGO B 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention relates to versatile linkers for tethering a molecule to a solid support, e.g., for tethering a monomer, oligomer or polymer to a solid support, which are stable to a wide range of reaction conditions, but can be cleaved under well-defined conditions, thereby liberating the molecule from the solid support. Preferably, the linkers are used to tether to the solid support unprotected, partially-protected or fully-protected monosaccharides or oligosaccharides, or unprotected, partially-protected or fully-protected glycoconjugates. The linkers of the present invention may be used to tether to solid supports building blocks useful in the assembly of libraries of other types of small molecules. The present invention also relates to a molecule or plurality of molecules tethered to the solid support via a linker or linkers of the present invention. The present invention also relates to processes for synthesizing molecules, e.g., monomers, oligomers or polymers, on a solid support, wherein a starting material in the synthesis of the molecule, intermediates in the synthesis of the molecule, and the molecule itself are tethered to the solid support during the process via one of the linkers of the present invention. In certain processes of the present invention, the molecule is liberated from the solid support by cleavage of the linker of the present invention.
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-2024317784-A1 优先权日:2021-07-13 标题 :Process for the synthesis of 4-((r)-2-{[6-((s)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester 发明人:BLUMER NICOLE; CLAVEAU ROMAIN; FEYEN FABIAN; HALL LEANNE; HUGHES STEPHEN; REBER STEFAN 权利人:VIATRIS ASIA PACIFIC PTE LTD 摘要:The present invention relates to a process for the synthesis of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester, or of a hydrochloride salt thereof; and to a crystalline form of 4-((R)-2-{[6-((S)-3-methoxy-pyrrolidin-1-yl)-2-phenyl-pyrimidine-4-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester hydrochloride.
专利号:US-7148356-B2 优先权日:2001-07-13 标题:Process for the catalytic synthesis of biaryls and polymers from aryl compounds 发明人:SMITH III MILTON R; MALECZKA ROBERT E 权利人:UNIV MICHIGAN STATE 摘要:A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or heteroaromatic compound is borylated in a reaction comprising a borane or diborane reagent (any boron reagent where the boron reagent contains a B—H, B—B or B—Si bond) and an iridium or rhodium catalytic complex. In the second step, a metal catalyst catalyzes the formation of the organic substituted aromatic or heteroaromatic compound from the borylated compound and an electrophile such as an aryl or organic halide, triflate (OSO 2 CF 3 ), or nonaflate (OSO 2 C 4 F 9 ). The steps in the process can be performed in a single reaction vessel or in separate reaction vessels. The present invention also provides a process for synthesis of complex polyphenylenes starting from halogenated aromatic compounds.
专利号:EP-3438097-A1 优先权日:2017-07-31 标 题:Synthesis of 2-(4-(trifluoromethyl)phenyl)-4h-benzo[d][1,3]oxazin-4-one from 1-(4-trifluoromethylbenzoyl)-1h-benzotriazole by adding palladiumchloride (pdcl2) and biphephos (6,6'-[(3,3'-di-tert-butyl-5,5'-dimethoxy-1,1'-biphenyl-2,2'-diyl)bis(oxy)]bis(dibenzo[d,f][1,3,2]dioxaphosphepine)) as well as similar processes 发明人:WU XIAO-FENG; YIN ZHIPING; QI XINXIN; BÖRNER ARMIN; FRANKE ROBERT 权利人:EVONIK DEGUSSA GMBH 摘要:Synthesis of 2- (4- (trifluoromethyl) phenyl) -4H-benzo [d] [1,3] oxazin-4-one from 1- (4-trifluoromethylbenzoyl) -1H-benzotriazole with addition of palladium chloride (PdCl2) and BiPhePhos (6,6 '- [(3,3'-di-tert-butyl-5,5'-dimethoxy-1,1'-biphenyl-2,2'-diyl) bis (oxy)] bis (dibenzo [d , f] [1,3,2] dioxaphosphepin)) and supply of carbon monoxide (CO) and similar processes for the preparation of 4H-benzo [d] [1,3] oxazin-4-one derivatives from 1-carbonyl-1H benzotriazole derivatives.
专利号:US-2007249867-A1 优先权日:2004-08-11 标题 :Method for Synthesis of Aromatic Amine 发明人:NAKASHIMA HARUE; KAWAKAMI SACHIKO 权利人:NAKASHIMA HARUE; KAWAKAMI SACHIKO 摘要:One embodiment of the present invention provides a method for synthesis of substituted secondary amine by the reaction of aniline with aryl halide by using a Pd catalyst including (t-Bu) 3 P as a ligand.