专利号:US-2023212788-A1 优先权日:2020-03-26 标 题:New method for automated on-demand biomolecular array synthesis 发明人:ZHANG YIXIN; LIN WEILIN 权利人:UNIV DRESDEN TECH 摘要:The invention provides an amphiphilic coating for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, comprising a hydrophilic chemical structure and a lipophilic group, wherein said peptides and small molecular compounds differ from spot to spot from each other in the chemical structure, characterized in that said amphiphilic coating possesses low wettability to polar aprotic solvents used in the array synthesis; said amphiphilic coating possessing low wettability is designed that it can be converted to a coating possessing high wettability by hydrolysis of the lipophilic group; and said amphiphilic coating comprises an amino group for the reaction with an electrophilic reagent. The invention further provides a solid support comprising said amphiphilic coating and a method for method for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, wherein said planar surface of a solid support comprises said amphiphilic coating. Said method includes the enhancing of the wettability of a glass surface to organic solvents to realize automated on-demand biomolecular array synthesis comprising both, peptides and small molecular compounds. The amphiphilic surface can be switched to a hydrophilic surface, resulting in high density arrays suitable for protein- and cell-based screening.
专利号:US-6858749-B2 优先权日:2000-02-04 标题:Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one 发明人:FLEMING MICHAEL P; HAN YEUN-KWEI; HODGES LEWIS M; JOHNSTON DAVID A; MICHELI ROGER P; PUENTENER KURT; ROBERTS CHRIS R; SCALONE MICHELANGELO; SCHWINDT MARK A; TOPPING ROBERT J 权利人:ROCHE COLORADO CORP 摘要:The present invention relates to a novel process for producing a delta-lactone of the formula:using an acyl halide of the formula:wherein R<1>, R<2 >R<3 >and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-delta-lactone.
专利号:US-6552204-B1 优先权日:2000-02-04 标 题 :Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one 发明人:HARRINGTON PETER J; HODGES LEWIS M; PUENTENER KURT; SCALONE MICHELANGELO 权利人:ROCHE COLORADO CORP 摘要:The present invention relates to a novel process for producing a δ-lactone of the formula: n using an acyl halide of the formula: n wherein R 1 , R 2 R 3 and X are described herein. In particular, the present invention relates to a process for enantioselectively producing the δ-lactone and novel intermediates disclosed herein.
专利号:US-10919921-B2 优先权日:2016-05-06 标题:P-chiral phosphine ligands and use thereof for asymmetric synthesis 发明人:BOERNER ARMIN; HOLZ JENS; RUMPEL KATHARINA 权利人:BASF SE 摘要:The present invention relates to chiral compounds with two optically active phosphorus atoms, chiral transition metal catalysts which comprise these compounds as ligands, a process for preparing the P-chiral compounds and processes for asymmetric synthesis using the chiral transition metal catalysts. The present invention specifically relates to a process for preparing an optically active carbonyl compound by asymmetric hydrogenation of a prochiral α,β-unsaturated carbonyl compound with hydrogen in the presence of an optically active transition metal catalyst according to the invention. Yet more specifically, the present invention relates to a process for the asymmetric hydrogenation of citral, and also a process for preparing optically active menthol.
专利号:US-12344592-B2 优先权日:2020-01-17 标题 :Methods, processes and intermediates for preparing chroman compounds 发明人:KAMBOJ RAJENDER KUMAR; PADIYA KAMLESH JYOTINDRA; PRABAKARAN KAMALAKANNAN; NAIK KUMAR RAM; RAJESH BHAVANI SHANKAR; RAJENDRA GANPATI POWAR; SACHIN SUBHASH INGAWALE; AMIT DATTATRAY KARCHE; SANTOSHKUMAR SHANKAR DANGE; SITARAM RAMBHAU BARVE 权利人:LUPIN LTD 摘要:This disclosure describes an economical and scalable method and process to synthesize the Calcium sensing receptor (CaSR) modulating agent 2-methyl-5-((2R,4S)-2-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)chroman-4-yl)benzoic acid, its intermediates and pharmaceutically acceptable salts therefor. Uses of said intermediates for synthesis of compounds which may be intermediates to the synthesis of 2-methyl-5-((2R,4S)-2-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)chroman-4-yl)benzoic acid are also described herein.
专利号:US-2003158422-A1 优先权日:2000-02-04 标 题:Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one