专利号:US-2023174567-A1 优先权日:2020-05-22 标题:Synthesis of fluorinated nucleotides 发明人:ARMIGER TRAVIS; BELYK KEVIN M; BENKOVICS TAMAS; CHUNG CHEOL K; JI CHEN YINING; JOHNSON HEATHER CLAIRE; KLAPARS ARTIS; LIU ZHIJIAN; LIU ZHUQING; MOORE JEFFREY C; NEEL ANDREW J; PENG FENG; RUMMELT STEPHAN M; SALEHI MARZUARANI NASTARAN; SHERRY BENJAMIN D; SONG ZHIGUO JAKE; TURNBULL BEN WILLIAM HULME; WANG LU; XU FENG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3′-fluoro-thio-guanosine monophosphate or 3′-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. (I)
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-5965719-A 优先权日:1996-11-15 标 题:Combinatorial synthesis of carbohydrate libraries 发明人:HINDSGAUL OLE 权利人:SUNSORB BIOTECH INC 摘要:Disclosed are methods for synthesizing very large collections of diverse thiosaccharide derivatives optionally attached to a solid support. Also disclosed are libraries of diverse thiosaccharide derivatives.
专利号:US-5300437-A 优先权日:1989-06-22 标 题 :Enantiomeric enrichment and stereoselective synthesis of chiral amines 发明人:STIRLING DAVID I; MATCHAM GEORGE W; ZEITLIN ANDREW L 权利人:CELGENE CORP 摘要:Amines in which the amino group is on a secondary carbon atom which is chirally substituted can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The process also can be used to stereoselectively synthesize one chiral form from ketones substantially to the exclusion of the other.
专利号:US-5169780-A 优先权日:1989-06-22 标题:Enantiomeric enrichment and stereoselective synthesis of chiral amines 发明人:STIRLING DAVID I; ZEITLIN ANDREW L; MATCHAM GEORGE W; ROZZELL JR JAMES D 权利人:CELGENE CORP 摘要:Amines in which the amino group is on a secondary carbon atom which is chirally substituted can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The process can be used to stereoselectively sythesize one chiral form from ketones substantially to the exclusion of the other. An aqueous solution of chiral amines after being brought into contact with an omega-amino acid transaminase and an amino acceptor is treated with a water-immiscible organic solvent, the aqueous and organic phases are separated, and the aqueous phase can be recirculated for further contact with the transaminase.
专利号:US-4950606-A 优先权日:1989-06-22 标题 :Enantiomeric enrichment and stereoselective synthesis of chiral amines 发明人:STIRLING DAVID I; ZEITLIN ANDREW L; MATCHAM GEORGE W 权利人:CELGENE CORP 摘要:Amines in which the amino group is on a secondary carbon atom which is chirally substituted can be enantiomerically enriched by the action of an omega-amino acid transaminase which has the property of preferentially converting one of the two chiral forms to a ketone. The process also can be used to stereoselectively synthesize one chiral form from ketones substantially to the exclusion of the other.