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-6867306-B2 优先权日:2001-01-19 标题:Process for the synthesis of atorvastatin form v and phenylboronates as intermediate compounds 发明人:SRINATH SUMITRA; MATHEW JOY; UJIRE SANDHYA; SRIDHARAN MADHAVAN; SAMBASIVAM GANESH 权利人:BIOCON LTD 摘要:The present invention discusses a novel process for the synthesis of [R-(R*,R*)]-2-(4-fluorophenyl)-B,D-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium, atorvastatin. The compound so prepared is useful as inhibitor of the HMG-CoA reductase and may thus be used as hypolipidemic and hypocholesterolemic agent.
专利号:US-2009197311-A1 优先权日:2006-06-20 标题:Method for the production of simvastatin 发明人:BERG MARCO ALEXANDER VAN DEN; HANS MARCUS; STREEKSTRA HUGO 权利人:BERG MARCO ALEXANDER VAN DEN; HANS MARCUS; STREEKSTRA HUGO 摘要:The present invention provides a fermentative process for the synthesis of simvastatin by providing a host capable of incorporating the 2,2-dimethylbutyrate side chain into simvastatin, i.e. by customizing a polyketide synthase gene optimized for synthesis and/or incorporation of 2,2-dimethylbutyrate; optionally feeding said host with the appropriate substrate for 2,2-dimethylbutyrate synthesis; fermenting said host to obtain simvastatin or analogues or derivatives thereof, i.e. by producing simvastatin on an industrial scale by a fed-batch process.
专利号:WO-2004031131-A1 优先权日:2002-10-03 标 题 :Improved syntheton synthesis 发明人:KWON TAESOO; GU CHEN; YANG SOON-HA 权利人:SK ENERGY AND CHEMICAL INC; KWON TAESOO; GU CHEN; YANG SOON-HA 摘要:The present disclosure relates to an improved synthesis of the commercially important syntheton ECHB starting from the readily available 3-hydroxy-Ïœ-butyrolactone. The reaction employs a single pot procedure without isolation or purification of the intermediates. It has the advantage over procedures previously employed in the art of using reagents and conditions which minimize undesired side reactions and which can be readily employed at commercial scale. The product is produced in high yield and is readily purified to provide an excellent intermediate for further synthesis of commercially important products such as L-carnitine and the pharmaceutically important active substances used in HMG-coA reductase inhibitor products such as Lipitorè.
专利号:US-6288244-B1 优先权日:1999-03-31 标 题 :Process for the preparation of 3, 4-dihydroxybutanoic acid and derivatives thereof from substituted pentose sugars 发明人:HOLLINGSWORTH RAWLE I 权利人:UNIV MICHIGAN STATE 摘要:A process for the preparation of 3,4-dihydroxybutanoic acid (I) and 3-hydroxy-γ-butyrolactone (V) thereof from a 3-leaving group substituted pentose source is described. In particular, the process relates to the synthesis of (R)-3,4-dihydroxybutanoic acid and (R)-3-hydroxy-γ-butyrolactone from a 3-leaving group substituted L-pentose sugars. The process uses a base and a peroxide to convert the pentose source to the chiral 3,4-dihydroxybutanoic acid compound. The chiral 3,4-dihydroxybutanoic acid can be further converted to 3-hydroxy-γ-butyrolactone by acidification. The chiral compound is useful as a chemical intermediate to the synthesis of various drugs and other products.
专利号:US-6096883-A 优先权日:1996-05-31 标 题 :3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones 发明人:WU GEORGE G; CHEN XING; WONG YEE-SHING; SCHUMACHER DORIS P; STEINMAN MARTIN 权利人:SCHERING CORP 摘要:The invention relates to intermediates of the formulae ##STR1## said intermediates being useful in a process for producing a compound of the formula ##STR2## wherein Bn is benzyl and R 1 , 2 and R 3 are as defined in the specification,