CAS: 209984-57-6; (S)-2-((S)-2-(3,5-Difluorophenyl)-2-Hydroxyacetamido)-N-((S)-5-Methyl-6-Oxo-6,7-Dihydro-5H-Dibenzo[b,D]Azepin-7-yl)Propanamide

结构式图片

上下游产品

7-(S)-(L-Alaninyl)-Amino-5-Methyl-5,7-Dihydro-6H-Dibenz[b,D]Azepin-6-One

合成工艺路线路线简述

    📜3,5-二氟苯甲醛置于n-碘代丁二酰亚胺,Cu(O-I-Bz)2*h2O,四磷十氧化物,Benzotriazol-1-Yloxyl-Tris-(Pyrrolidino)-Phosphonium Hexafluorophosphate,水,双氧水,氧气,Potassium Carbonate,(S,S)-(-)-2,2'-异亚丙基双(4-叔丁基-2-恶唑啉),1-羟基苯并三唑,N,N-二异丙基乙胺,三氟乙酸,Lithium Hydroxide体系中,用 四氢呋喃,2-甲基四氢呋喃,二氯甲烷,氯仿,水,异丙醇 用作溶剂,化学反应 159.08H,反应生成(As)-N-[(1S)-2-[[(7S)-6,7-二氢-5-甲基-6-氧代-5H-二苯并[b,D]氮杂卓-7-基]氨基]-1-甲基-2-氧代乙基]-3,5-二氟-Alpha-羟基苯乙酰胺
    参考文献:通过 Umpolung 酰胺合成对映选择性合成 α-氧酰胺
    标题:通过 Umpolung 酰胺合成对映选择性合成 α-氧酰胺
    摘要:α-氧酰胺是通过对映选择性合成制备的,使用的序列从溴硝基甲烷与醛的亨利加成开始,最后是 Umpolung 酰胺合成 (Umas).高对映体选择的关键是发现手性铜 (II) 双(恶唑啉) 催化剂的邻碘苯甲酸盐提供亨利加合物的两种非对映异构体,对映体过量,在含氧碳上同手性.总体而言,这种 α-氧基酰胺方法为几乎完全专注于 α-氧基羧酸的对映选择性合成的替代品提供了创新的补充.
    Doi:10.1021/ja306225U

    海关参考信息

    专利信息


    专利号:US-6486350-B1
    优先权日:1998-09-30
    标 题:Biological reagents and methods for determining the mechanism in the generation of β-amyloid peptide
    发明人:AUDIA JAMES E; HYSLOP PAUL A; NISSEN JEFFREY S; THOMPSON RICHARD C; TUNG JAY S; TANNER LAURA I
    权利人:ELAN PHARM INC; LILLY CO ELI
    摘要:Disclosed are biological reagents which comprise compounds that inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in determining the cellular mechanism involved in the generation of beta-amyloid peptide.

    专利号:EP-2546229-A1
    优先权日:2011-07-15
    标 题:Method for synthesising aminobiphenyls
    发明人:HEINRICH MARKUS; PRATSCH GERALD
    权利人:UNIV FRIEDRICH ALEXANDER ER
    摘要:The present invention describes a process for the synthesis of 2-aminobiphenyls and derivatives thereof. This method is inexpensive to carry out and based on selective implementation. Functionalized biphenyl compounds are of great interest in particular as pharmaceuticals and crop protection agents and as precursors of such active substances. The process for preparing a compound of formula 3 is characterized in that a compound of formula 1 is reacted with a compound of formula 2.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Liu-Seifert H, Siemers E, Price K, Han B, Selzler KJ, Henley D, Sundell K, Aisen P, Cummings J, Raskin J, Mohs R; Alzheimer’s Disease Neuroimaging Initiative. Cognitive Impairment Precedes and Predicts Functional Impairment in Mild Alzheimer's Disease. J Alzheimers Dis. 2015;47(1):205-14. doi: 10.3233/JAD-142508.
    2: Ran Y, Ladd GZ, Ceballos-Diaz C, Jung JI, Greenbaum D, Felsenstein KM, Golde TE. Differential Inhibition of Signal Peptide Peptidase Family Members by Established γ-Secretase Inhibitors. PLoS One. 2015 Jun 5;10(6):e0128619. doi: 10.1371/journal.pone.0128619. eCollection 2015.
    3: De Strooper B. Lessons from a failed γ-secretase Alzheimer trial. Cell. 2014 Nov 6;159(4):721-6. doi: 10.1016/j.cell.2014.10.016. doi: 10.1146/annurev-pharmtox-010814-124309. Epub 2014 Oct 1. Review. doi: 10.1001/jamaneurol.2014.2482.

    合成参考文献


    参考文献:10.1038/475s9a
    摘要:Gravitz L. Drugs: a tangled web of targets. Nature. 2011 Jul 13;475(7355):S9–11. doi: 10.1038/475s9a.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知