CAS: 198904-31-3; 1,14-Dimethyl (3S,8S,9S,12S)-3,12-Bis(1,1-Dimethylethyl)-8-Hydroxy-4,11-Dioxo-9-(Phenylmethyl)-6-[[4-(2-Pyridinyl)Phenyl]Methyl]-2,5,6,10,13-Pentaazatetradecanedioate

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(S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoic acid 1-[4-(pyridin-2-yl)phenyl]-4(S)-hydroxy-5(S)-2,5-diamino-6-phenyl-2-azahexane trihydr°Chloride {(S)-1-[N'-((2S,3S)-3-amino-2-hydroxy-4-phenyl-butyl)-N'-(4-pyridin-2-yl-benzyl)-hydrazin°Carbonyl]-2,2-dimethyl-propyl}-carbamic acid methyl ester 1-(4-(pyridin-2-yl)benzyl)hydrazine45H63F2N9O7C45H63F2N9O7 45H63F2N9O7C45H63F2N9O7

4-溴苯甲醛二甲缩醛置于盐酸,10 Wt% Pd(Oh)2 On Carbon,氢气,碘,Magnesium,Lithium Tri-T-Butoxyaluminum Hydride,三乙胺,Sodium Iodide体系中,用 四氢呋喃,乙醚,乙醇,水,乙腈 用作溶剂,20.0 °C,101.33 Kpa 条件下,反应 25.75H,反应生成阿扎那韦
参考文献:通过高度非对映选择性还原方法高效,实用地合成hiv蛋白酶抑制剂atazanavir
标题:通过高度非对映选择性还原方法高效,实用地合成hiv蛋白酶抑制剂atazanavir
摘要:通过采用非对映选择性还原酮亚甲基氮杂-二肽等排物10作为关键和最终步骤,开发了一种有效且实用的hiv-1蛋白酶抑制剂atazanavir合成方法.通过felkin-Anh控制,由于笨重和手性的n-(-)的结果,通过三叔丁氧基氢化铝锂在乙醚中还原氨基酮的高非对映选择性,从而得到所需的顺式1,2-氨基醇结构.甲氧基羰基)-升-叔-Leucinyl部分为氮保护基团.两个关键中间体的联接器,ñ-(甲氧羰基)-升-叔亮氨酸酰化的苄基肼7和氯甲基酮9通过s N 2反应在我们优化的条件下以高收率提供了氨基酮10.我们的新方法提供了引入末的小号羟基基团和苄基肼和氯甲基酮与早期酰化ñ-(甲氧羰基)-升-叔-亮氨酸,分别,其赋予高效率和容易纯化.
Doi:10.1021/op7001563

专利信息

专利号:US-10889599-B2
优先权日:2018-02-27
标 题:1,1-diborylalkyl-1-metal compounds, preparation method thereof, and their applications toward synthesis of 1,1-diboronate ester compounds
发明人：CHO SEUNG HWAN; LEE YEOSAN
权利人:POSTECH ACAD IND FOUND
摘要:The present invention relates to a 1,1-diborylalkyl-1-metal compound including one metal group together with two identical boron groups at the sp3 carbon center, and its use. Specifically, the present invention relates to development of novel organic reactions, synthesis of functional molecules, and synthesis of new drugs by applying the novel 1,1-diboryl-1-metal substituted alkyl compounds to various molecular libraries which could not be synthesized by conventional methodologies.

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-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

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.