专利号:US-5849936-A 优先权日:1995-03-15 标题:Method for the synthesis of bis-tetrahydrofuranyl annonaceous acetogenins 发明人:HOYE THOMAS R; TAN LUSHI 权利人:UNIVERISTY OF MINNESOTA 摘要:A method for the synthesis of bis-tetrahydrofranyl Annonaceous acetogenins, including the natural products and analogs thereof, is provided which proceeds by the Pd-mediated coupling of a bis-tetrahydrofuranyl-subunit comprising a terminal alkyne, with a (C4)-hydroxybutenolide subunit comprising a terminal vinyl iodide, followed by selective reduction of the resulting enyne.
专利号:US-9233943-B2 优先权日:2012-01-10 标题:Process for synthesis of syn azido epdxide and its use as intermediate for the synthesis of amprenavir and saquinavir 发明人:GADAKH SUNITA KHANDERAO; REKULA REDDY SANTHOSH; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:A novel synthetic route to the syn-azido epoxide of formula 5 includes cobalt-catalyzed hydrolytic kinetic resolution of a racemic mixture of the azido-epoxide. Reaction steps include subjecting an allylic alcohol to epoxidation with mCPBA to obtain a racemic epoxy alcohol; ring opening the epoxy alcohol with azide anion to obtain an anti-azido alcohol, which can then be selectively tosylated at the primary alcohol; treating the tosylate with base to obtain the racemic azido-epoxide; and subjecting the racemic azido-epoxide to cobalt-catalyzed hydrolytic kinetic resolution to obtain the syn-azido epoxide of formula 5. The compound of formula 5 may be used as a common intermediate for the asymmetric synthesis of HIV protease inhibitors, such as Amprenavir, Fosamprenavir, Saquinavir, and formal synthesis of Darunavir and Palinavir.
专利号:US-2018297925-A1 优先权日:2015-10-12 标题 :Methods for total synthesis of resolvin e1 发明人:JAGTAP PRAKASH 权利人:SALZMAN LOVELACE INVEST LTD 摘要:Methods for total chemical synthesis of Resolvin E1 (RvE1) include Wittig reaction of two compounds having hydroxyl protecting group in the presence of a strong base, removal of the hydroxyl-protecting groups with a deprotecting reagent to produce a compound having an ester group, and hydrolysis of the ester group to obtain RvE1
专利号:US-6849743-B2 优先权日:1997-08-15 标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof 发明人:SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM 权利人:MILLENNIUM PHARM INC 摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.
专利号:US-9809566-B2 优先权日:2012-09-06 标题:Organocatalytic process for asymmetric synthesis of decanolides 发明人:RAWAT VARUN; DEY SOUMEN; SHELKE ANIL MARUTI; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.
专利号:US-8314090-B2 优先权日:2008-11-06 标 题:Methods of synthesis of benzazepine derivatives 发明人:HOWBERT J JEFFRY; KUSUKUNTLA VENKAT REDDY; TRETYAKOV ALEXANDER; NIELSEN NATHAN; KRASIK PAVEL; JIANG JI-LONG; YANG HONG WOON 权利人:HOWBERT J JEFFRY; KUSUKUNTLA VENKAT REDDY; TRETYAKOV ALEXANDER; NIELSEN NATHAN; KRASIK PAVEL; JIANG JI-LONG; YANG HONG WOON; VENTIRX PHARMACEUTICALS INC; ARRAY BIOPHARMA INC 摘要:The disclosure describes method of synthesis of substituted benzazepine derivatives. Preferred methods according to the disclosure allow for large-scale preparation of benzazepine compounds having low levels of metal impurities. In some embodiments, preferred methods according to the disclosure also allow for the preparation of benzazepine derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.
参考标题:Process For Synthesis Of Syn Azido Epoxide And Its Use As Intermediate For The Synthesis Of Amprenavir & Saquinavir 摘要:Disclosed Herein Is A Novel Route Of Synthesis Of Syn Azide Epoxide Of Formula 5, Which Is Used As A Common Intermediate For Asymmetric Synthesis Of Hiv Protease Inhibitors Such As Amprenavir, Fosamprenavir, Saquinavir And Formal Synthesis Of Darunavir And Palinavir Obtained By Cobalt-Catalyzed Hydrolytic Kinetic Resolution Of Racemic Anti-(2Sr,3Sr)-3-Azido-4-Phenyl-1,2-Epoxybutane (Azido-Epoxide).
合成参考文献
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