专利号:WO-8800592-A1 优先权日:1986-07-18 标题:DIASTEROSELECTIVE STRECKER SYNTHESIS OF alpha-AMINOACIDS FROM GLYCOSYLAMINE DERIVATES 发明人:KUNZ HORST; SAGER WILFRIED; PFRENGE WALDEMAR; DECKER MATHIAS 权利人:CELAMERCK GMBH & CO KG 摘要:O-acyl-protected glycosylamines, in particular 2,3,4,6-tetra-O-pivaloyl-beta-D-galactopyranosylamine (1), their preparation and their use for the diastereoselective synthesis of alpha-aminoacids. With compounds such as (1), one can obtain by Strecker synthesis high yields and high diastereomer surplus. The direction of the asymmetric induction can be determined by the selection of the solvent. This type of synthesis is particularly effective when carried with Lewis acid catalysts. One obtains also high yields and high diastereoselectivity during Ugi four component synthesis facilitated by Lewis acids by using amines such as (1).
专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:US-2002019013-A1 优先权日:1999-03-08 标 题:Combined resin method for high-speed synthesis of combinatorial libraries 发明人:LOU BOLIANG; GHARBAOUI TAWFIK 摘要:A method for high-speed parallel synthesis of combinatorial libraries is disclosed where two or more resins of dissimilar functionality are combined in the same reaction vessel in which a plurality of chemical reactions are carried out to create multiple compounds which are then sequentially and individually cleaved from the different resins under the appropriate cleavage conditions for each resin. As used herein resins are considered different when they exhibit different chemical activity in the presence of cleaving or releasing agents. The resins are different when the individual resins have either dissimilar polymeric backbones or dissimilar linkers or both and thus have a different chemical activity in the presence of a release or cleaving agent from the other resins in the reaction vessel.
专利号:WO-2016122325-A1 优先权日:2015-01-30 标 题:Methods for providing intermediates in the synthesis of atorvastatin. 发明人:DÖMLING ALEXANDER STEPHAN SIEGFRIED 权利人:UNIV GRONINGEN 摘要:The invention relates to the field of medicinal chemistry, In particular, it relates to methods for providing intermediates in the synthesis of Atorvastatin, a competitive inhibitor of HMG-Co A reductase. Provided is a process for providing a compound having a Formula (I) or a pharmaceutically acceptable salt, ester, amide or stereoisomer thereof, comprising reacting in a 4 component Ugi-reaction in a single reaction mixture the compounds of formula A, formula B, formula C and formula D.
专利号:US-6600016-B1 优先权日:1999-08-24 标题:Multifunctionalized solid support resins for synthesis of combinatorial libraries and method for using the same 发明人:CAMPIAN EUGENE; LU BOLIANG; ZHANG JINFANG 权利人:ADVANCED SYNTECH LLC 摘要:Multifunctionalized support resin for the solid phase synthesis of combinatorial libraries is disclosed. The support resin comprises a resin backbone to which is attached a template containing at least two more attachment points which carry mutiple functionalized benzyl-type linkers. Each linker displays differing chemical stability under cleavage conditions so that products can be selectively and sequentially cleaved and separated from the reaction vessel. The linkers are independently different benzyl-type moieties, and each product synthesized on the linkers may have a different chemical structure. The support resin may further comprise an additional linker which is directly attached to the resin backbone. This linker can benzyl-type linkers or other traditional cleavable-linkers. The invention is further directed to a method for the production of mutiple combinatorial libraries in a simultaneous fashion utilizing the above described support resin. The products are selectively cleaved under conditions where only one linker site is cleaved so that the product is individually separated from the reaction vessel.
专利号:US-2017320908-A1 优先权日:2014-11-19 标题 :Solid phase synthesis of cyclic amino acid molecules 发明人:HICKEY JENNIFER L; MANCUSO JOHN; MARSAULT ERIC; ROUGHTON ANDREW L; TREDER ADAM P; TREMBLEY MARIE-CLAUDE J; YUDIN ANDREI K; ZARETSKY SERGE 权利人:ENCYCLE THERAPEUTICS; GOVERNING COUNCIL OF THE UNIV OF TORONTO; UNIV SHERBROOKE 摘要:The present invention relates to cyclic amino acid molecules and methods of preparing the same, and in particular the macrocyclization of amino acids or linear peptides bound to a solid support.