专利号:US-8124790-B2 优先权日:2008-01-02 标题:Preparation process useful in synthesis of atorvastatin 发明人:CHO DONG-OCK; KWON YOUNJA; CHA KYEONG-HOI; KIM YEONGSOOK; TAE HYUN-SEOP 权利人:CHO DONG-OCK; KWON YOUNJA; CHA KYEONG-HOI; KIM YEONGSOOK; TAE HYUN-SEOP; MEDICHEM KOREA CO LTD 摘要:The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t-butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.
专利号:WO-0172706-A1 优先权日:2000-03-28 标题 :Synthesis of [r-(r*,r*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-heptanoic acid hemi calcium salt (atorvastatin) 发明人:SAMBASIVAN GANESH; SRIDHARAN MADHAVAN; PADUDEVASTANA SATHYASHANKER; POORNAPRAJNA ACHARYA; MATHEW JOY; SRINATH SUMITHRA; NAIR SATHEESH 权利人:BIOCON LTD; SAMBASIVAN GANESH; SRIDHARAN MADHAVAN; PADUDEVASTANA SATHYASHANKER; POORNAPRAJNA ACHARYA; MATHEW JOY; SRINATH SUMITHRA; NAIR SATHEESH 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 salt by using 4-fluoro-α-[2-methyl-1-oxopropyl]η-oxo-N-β-diphenylbenzene butaneamide with (4R)-methyl 6-(2-aminoethyl)-2,2-dimethyl-1,3-dioxane-3-acetate. The compound so prepared is useful as inhibitors of the enzyme HMG-CoA reductase and are thus used as hypolipidemic and hypocholesterolemic agents.
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-7399773-B2 优先权日:2001-01-09 标 题 :Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid and phenylamide 发明人:NELSON JADE DOUGLAS; PAMMENT MICHAEL GERARD 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.
专利号:US-8026383-B2 优先权日:2001-07-06 标题:Process for the preparation of intermediates useful in the synthesis of statin derivatives 发明人:OEHRLEIN REINHOLD; BAISCH GABRIELE; END NICOLE; BURKHARDT STEPHAN; STUDER MARTIN 权利人:BASF SE 摘要:The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I n nwherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH 3 )OCH 3 , R a is a hydroxy-protecting group and R b is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
专利号:US-2011263870-A1 优先权日:2010-04-23 标题 :Novel pyrrole derivatives and their synthesis 发明人:PRADHAN BRAJA SUNDAR 权利人:HELVETICA IND P LTD 摘要:The present invention relates to two novel pyrrole derivatives [3-Phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrole-1-yl]methyl(diphenyl)phosphine oxide and Diethyl [3-Phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrole-1-yl]methylphosphonate. These pyrrole derivatives can be used as intermediates for the synthesis of the anticholesterol drug atorvastatin.