CAS: 161814-49-9; (S)-Tetrahydrofuran-3-Yl ((2S,3R)-4-((4-Amino-N-Isobutylphenyl)Sulfonamido)-3-Hydroxy-1-Phenylbutan-2-yl)Carbamate

上下游产品

1-({[(3S)-tetrahydro-3-furanyloxy]carbonyl}oxy)-2,5-pyrrolidinedione 4-amino-N-(2R,3S)(3-amino-2-hydroxy-4-phenylbutyl)-N-isobutylbenzenesulfonamide 4-nitro-N-((2R(syn),3S)-2-hydroxy-4-phenyl-3-((S)-tetrahydrofuran-3-yloxycarbonylamino)-butyl)-N-isobutylbenzenesulfonamide (1-oxiranyl-2-phenylethyl)carbamic acid tert-butyl ester

[(1S,2R)-1-苄基-2-羟基-3-[异丁基[(4-硝基苯基)磺酰]氨基]丙基]氨基甲酸叔丁酯置于盐酸,Tin(Ll) Chloride体系中,用 二氯甲烷,乙酸乙酯 用作溶剂,化学反应 8.5H,反应生成安普那韦
参考文献:合成手性氮丙啶衍生物作为hiv蛋白酶抑制剂的通用中间体.
标题:合成手性氮丙啶衍生物作为hiv蛋白酶抑制剂的通用中间体.
摘要:[反应:见正文]由d-酒石酸制备手性氮丙啶衍生物1.该化合物可以用作合成羟乙胺类hiv蛋白酶抑制剂(如沙奎那韦,氨普那韦或奈非那韦)的常用中间体.
Doi:10.1021/ol016147S

专利信息

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-6818633-B2
优先权日:2001-06-29
标题:Antiviral compounds and methods for synthesis and therapy
发明人：BALZARINI JAN M R; DE CLERCQ ERIK D A; HOLY ANTONIN
权利人:ACAD OF SCIENCE CZECH REPUBLIC; REGA STICHTING
摘要:Novel compounds are provided having formula (I)whereR1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).

专利号:US-8987493-B2
优先权日:2010-05-20
标题 :Process for synthesis of silane dipeptide analogs
发明人：SIEBURTH SCOTT MCNEILL; BO YINGJIAN
权利人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN; Temple University—Of the Commonwealth System of Higher Education
摘要:The invention provides a method of preparing silane dipeptide analogs, comprising the steps of treating a solution of a substituted 1,2-oxasilolane with lithium metal to form a solution of the dilithium salt of a substituted 3-hydroxypropylsilanol, and reacting the solution of the dilithium salt of the substituted 3-hydroxypropylsilanol with a substituted enamine.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-11845970-B2
优先权日:2016-01-15
标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins
发明人：WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN
权利人:UNIV MARYLAND
摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.