CAS: 159989-64-7; (3S,4As,8As)-N-(Tert-Butyl)-2-((2R,3R)-2-Hydroxy-3-(3-Hydroxy-2-Methylbenzamido)-4-(Phenylthio)Butyl)Decahydroisoquinoline-3-Carboxamide

上下游产品

thiophenol (3S,4aS,8aS)-N-tert-butyl-2-((R)-2-hydroxy-2-((S)-2-(3-hydroxy-2-methylphenyl)-4,5-dihydrooxazol-4-yl)ethyl)-decahydroisoquinoline-3-carboxamide 3-acetoxy-2-methylbenzoyl chloride (2R,3R)-4-((3S,4aS,8aS)-3-(tertbutylcarbamoyl)°Ctahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-(phenylthio)butan-2-aminium benzoatenelfinavir mesylate

2-甲基-3-乙酰氧基苯甲酸置于盐酸,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺,对甲苯磺酰氯体系中,用 甲醇 用作溶剂,化学反应 3.0H,反应生成奈非那韦
参考文献:A Short Synthesis Of The Hiv-Protease Inhibitor Nelfinavir Via A Diastereoselective Addition Of Ammonia To The α,β-Unsaturated Sulfoxide Derived From ( R )-Glyceraldehyde Acetonide
标题:A Short Synthesis Of The Hiv-Protease Inhibitor Nelfinavir Via A Diastereoselective Addition Of Ammonia To The α,β-Unsaturated Sulfoxide Derived From ( R )-Glyceraldehyde Acetonide
摘要:Diastereoselective Michael Addition Of Ammonia To Sulfoxide 3A Derived From (R)-Glyceraldehyde Acetonide Provides Amine 4A,Which Is Converted Into Nelfinavir Using (Bf3Et2O)-Et-./nal Reduction And Subsequent Coupling Reactions As Key Steps. (C) 2002 Elsevier Science Ltd. All Rights Reserved.
Doi:10.1016/s0040-4039(02)02077-4

专利信息

专利号:US-7173059-B2
优先权日:2003-05-08
标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same
发明人：ALBIZATI KIM FRANCIS; BABU SRINIVASAN
权利人:AGOURON PHARMA
摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.

专利号:US-6472534-B2
优先权日:1999-10-21
标 题:Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors
发明人：BORER BENNETT C; ZOOK SCOTT E; BUSSE JULIETTE K
权利人:AGOURON PHARMA
摘要:Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.

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-2010261876-A1
优先权日:2007-09-25
标 题:Novel methods of synthesis for therapeutic antiviral peptides
发明人：BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E
权利人:BRAY BRIAN L; JOHNSTON BARBARA E; SCHNEIDER STEPHEN E; TVERMOES NICOLAI A; ZHANG HUYI; FRIEDRICH PAUL E
摘要:Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.

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.