(R)-(-)-3-羟基四氢呋喃置于bis(2-Methoxyethyl) Azodicarboxylate,4-二苯基膦苯甲酸,水,Sodium Hydroxide体系中,用 四氢呋喃 作为反应溶剂,化学反应 0.17H,以64%的收率获得产物(S)-3-羟基四氢呋喃 参考文献:Mitsunobu Reaction With 4-(Diphenylphosphino)Benzoic Acid: A Separation-Friendly Bifunctional Reagent That Serves As Both A Reductant And A Pronucleophile 标题:Mitsunobu Reaction With 4-(Diphenylphosphino)Benzoic Acid: A Separation-Friendly Bifunctional Reagent That Serves As Both A Reductant And A Pronucleophile 摘要:4-(Diphenylphosphino)Benzoic Acid Was Used For The Mitsunobu Reaction As A Bifunctional Reagent That Served As Both A Reductant And A Pronucleophile. When Combined With Di-2-Methoxyethyl Azodicarboxylate,Inversion Of A Secondary Alcohol Stereospecifically occurred To Give An Ester Carrying A Phosphine Oxide Group. The Reaction Mixture Was Directly Hydrolyzed To Give An Inverted Secondary Alcohol In Sufficient Stereo And Chemical Purities By The Presently Developed Chromatography-Free Process In Conjunction With Basic Extraction,Drying,And Concentration. DOI:10.1055/s-0032-1318327
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
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-6281367-B1 优先权日:1998-03-20 标 题:Process for the synthesis of HIV protease inhibitors 发明人:AL-FARHAN EMILE; DEININGER DAVID D; MCGHIE STEPHEN; O'CALLAGHAN JOHN; ROBERTSON MARK STUART; RODGERS KEITH; ROUT STEPHEN JOHN; SINGH HARDEW; TUNG ROGER DENNIS 权利人:GLAXO WELLCOME INC 摘要:An improved process for the synthesis of (3S)-tetrahydro-3-furyl N-[(1S,2R)-3 -(4-amino-N-isobutylbenzenesulphonamido)-1-benzyl-2-hydroxypropyl]carbamate comprising four steps form the compound of formula A and a novel intermediate thereto.
专利号:US-10988473-B2 优先权日:2016-10-25 标题 :Process for the preparation of (3S,4S)-tetrahydrofuran-3-yl 4-isopropyl-6,7-dihydro-3H-imidazo[4,5-C]pyridine-5(4H)-carboxylate 发明人:HORGAN VIET-ANH ANNE; HAGLUND OLOF; PATIENT LEE; SAVORY EDWARD; HIGGINBOTTOM MICHAEL; ASHWOOD MICHAEL 权利人:BENEVOLENTAI CAMBRIDGE LTD; BENEVOLENTAL CAMBRIDGE LTD 摘要:The invention relates to an improved process for the synthesis of (3S, 4S)-tetrahydrofuran-3-yl 4-isopropyl-6,7-dihydro-3H-imidazo[4,5-c]pyridine-5(4H)-carboxylate, and pharmaceutically acceptable salts thereof, such as the methanesulphonic acid salt.
专利号:US-9045462-B2 优先权日:2012-08-17 标 题 :Synthesis of an antiviral compound 发明人:EVANS JARED WAYNE; FUJIMORI SHINJI; HUYNH GRACE M; LIU QI; TERESK MARTIN GERALD 权利人:GILEAD SCIENCES INC 摘要:The present disclosure provides processes for the preparation of a compound of Formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
专利号:US-7514573-B2 优先权日:2007-04-11 标题:Processes for the manufacture of chiral and racemic forms of 3-aminotetrahydrofurans, their salts and derivatives 发明人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; BALAKRISHNAN SIVAPRSKASH KURUMANGHAT; GANJIHAL SAVITA; RAMANUJAM RAJENDRAN; SOOD RATTAN; PRAKASH SUBBALAKSHMI 权利人:SAMI LABS LTD 摘要:A novel process for the synthesis of (S)-3-Amino-tetrahydrofuran and (R)-3-Amino-tetrahydrofuran is described. The process is applicable for substituted chiral-3-aminotetrahydrofuran derivatives.