专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:US-9034844-B2 优先权日:2009-04-06 标 题 :6′-sialyllactose salts and process for their synthesis and for the synthesis of other alpha-sialyloligosaccharides 发明人:TAMERLANI GIANCARLO; LOMBARDI ILARIA; BARTALUCCI DEBORA; DANESI ANDREA; SALSINI LIANA; MANONI MARCO; CIPOLLETTI GIOVANNI 权利人:TAMERLANI GIANCARLO; LOMBARDI ILARIA; BARTALUCCI DEBORA; DANESI ANDREA; SALSINI LIANA; MANONI MARCO; CIPOLLETTI GIOVANNI; INALCO SPA 摘要:The present invention relates to a process of synthesis of α-sialyl oligosaccharides and in particular of 6′-sialyllactose and its salts comprising a step of coupling by Koenigs-Knorr reaction under conditions that allow its use on an industrial scale.
专利号:WO-9616071-A1 优先权日:1994-11-21 标题:PROCESSES FOR THE SYNTHESIS OF 3'-SUBSTITUTED LEWISx COMPOUNDS 发明人:SRIVASTAVA OM; IPPOLITO ROBERT; SRIVASTAVA GEETA; SZWEDA ROMAN; OHUCHI TOSHIO 权利人:GLYCOMED INC; SRIVASTAVA OM; IPPOLITO ROBERT; SRIVASTAVA GEETA; SZWEDA ROMAN; OHUCHI TOSHIO 摘要:Disclosed are processes for the chemical synthesis of 3'-substituted Lewis-OR compounds where R is an aglycon of at least one carbon atom. One particular compound prepared by the processes of this invention is 8-methoxycarbonyl-octyl-2-acetamido-3-O-( alpha -L-fucopyranosyl)-4-O-[3-O-sulfo- beta -D-galactopyranosyl]-2-deoxy- beta -D-glucopyranoside.
专利号:US-5338865-A 优先权日:1992-03-12 标 题 :Synthesis of halichondrin B and norhalichondrin B 发明人:KISHI YOSHITO; FANG FRANCIS; FORSYTH CRAIG J; SCOLA PAULA M; YOON SUK KYOON 权利人:HARVARD COLLEGE 摘要:Novel chemical compounds that can be used to synthesize halichondrin B and norhalichondrin B, and related derivatives, are described. The synthesis of halichondrin B and norhalichondrin B from these compounds also is described.
专利号:US-11306157-B2 优先权日:2018-12-21 标 题:Expedient synthesis of core disaccharide building blocks from natural polysaccharides for heparan sulfate oligosaccharide assembly 发明人:HSIEH-WILSON LINDA C; PAWAR NITIN J; WANG LEI 权利人:CALIFORNIA INST OF TECHN 摘要:Methods for the preparation of oligosaccharide products from polysaccharide starting materials are disclosed. The methods include: hydrolyzing a glucosamine-containing polysaccharide starting material, such as heparin or heparosan, under conditions sufficient to form an oligosaccharide intermediate (e.g., a GlcN-IdoA disaccharide intermediate or a GlcA-GlcN disaccharide intermediate), and converting the oligosaccharide intermediate to the oligosaccharide product. Conversion of the oligosaccharide intermediates to the oligosaccharide products may include one or more esterification, acylation, epimerization, protection, and deprotection steps. Preparation of higher-order oligomers is described, as well as methods for selective oligosaccharide sulfation.
专利号:US-11155562-B2 优先权日:2014-06-30 标 题 :Synthesis of halichondrin analogs and uses thereof 发明人:KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE 权利人:HARVARD COLLEGE 摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
参考标题:Total Synthesis Of The Macrolide Antibiotic Cytovaricin 作者:David A. Evans,Stephen W. Kaldor,Todd K. Jones,Jon Clardy,Thomas J. Stout |发布日期:1990.9 摘要:A Convergent Asymmetric Synthesis Of The Antinoeplastic Macrolide Antibiotic Cytovaricin Has Been Achieved Through The Synthesis And Coupling Of The Illustrated Spiroketal And Polyol Glycoside Subunits. All Absolute Steroechemical Relationships Within The Target Structure Were Ultimately Controlled By The Use Of Asymmetric Aldol, Alkylation, Or Epoxidation Methodology. Union Of The Two Subnits Was
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