1-trityloxy-5-tosyloxypentane

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 1-trityloxy-5-tosyloxypentane
• 英文别名: 5-Trityloxypentyl 4-methylbenzenesulfonate
• 化学式: C₃₁H₃₂O₄S
• 分子量: 500.659
• InChiKey: ZDUNXQXGFBDLNZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.2
• 重原子数：
  36
• 可旋转键数：
  12
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  61
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-trityloxy-5-tosyloxypentane 在 sodium hydride 、 过碘酸 、 对甲苯磺酰氯 、 pyridinium chlorochromate 作用下， 以 四氢呋喃 、 甲醇 、 乙腈 、 mineral oil 为溶剂， 反应 48.25h， 生成 6-氧杂-十一烷二酸
  参考文献：
  名称：

  DEZOCINE ANALOGUE

  摘要：

  公开号：

  EP3401306B1
• 作为产物：
  描述：

  三苯基氯甲烷 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 二氯甲烷 、 乙酸乙酯 为溶剂， 反应 5.0h， 生成 1-trityloxy-5-tosyloxypentane
  参考文献：
  名称：

  基于荧光偏振活性的蛋白质谱分析法在人类非溶酶体葡萄糖基神经酰胺酶的有效，选择性抑制剂的发现中。

  摘要：

  人非溶酶体葡萄糖基神经酰胺酶（GBA2）是控制糖脂水平的几种酶之一，其活性与几种人类疾病状态相关。迫切需要设计或发现选择性的GBA2抑制剂作为化学工具和潜在的治疗剂。在这里，我们描述了基于荧光偏振活性的蛋白质谱分析（FluoPol-ABPP）测定法的发展，该测定法可从350多种亚氨基糖文库中快速鉴定GBA2抑制剂。基于FluoPol-ABPP筛选的线索生成聚焦库，并针对与其他葡糖神经酰胺代谢酶，葡糖神经酰胺合酶（GCS），溶酶体葡糖神经酰胺酶（GBA）和胞质保留β-葡糖苷酶GBA3的GBA2选择性偏移进行评估。我们的工作产生了有效的和选择性的GBA2抑制剂，

  DOI：

  10.1021/jacs.7b07352

文献信息

• Highly Efficient Synthesis of Monodisperse Poly(ethylene glycols) and Derivatives through Macrocyclization of Oligo(ethylene glycols)
  作者：Hua Zhang、Xuefei Li、Qiuyan Shi、Yu Li、Guiquan Xia、Long Chen、Zhigang Yang、Zhong-Xing Jiang

  DOI：10.1002/anie.201410309

  日期：2015.3.16

  A macrocyclic sulfate (MCS)‐based approach to monodisperse poly(ethylene glycols) (M‐PEGs) and their monofunctionalized derivatives has been developed. Macrocyclization of oligo(ethylene glycols) (OEGs) provides MCS (up to a 62‐membered macrocycle) as versatile precursors for a range of monofunctionalized M‐PEGs. Through iterative nucleophilic ring‐opening reactions of MCS without performing group

  已开发出一种基于大环硫酸盐（MCS）的单分散聚乙二醇（M-PEG）及其单官能化衍生物的方法。寡聚乙二醇（OEG）的大环化提供了MCS（最多62个成员的大环），作为一系列单官能化M-PEG的通用前体。通过MCS的反复亲核开环反应而无需进行基团保护和激活，可以轻松制备一系列M-PEG，包括史无前例的64-mer（2850 Da）。合成简单性与这种新策略的多功能性可能为M-PEG的更广泛应用铺平道路。
• [EN] INHIBITORS OF CYCLIN-DEPENDENT KINASES AND USES THEREOF<br/>[FR] INHIBITEURS DE KINASES DÉPENDANTES DES CYCLINES ET LEURS UTILISATIONS
  申请人：LES LABORATOIRES SERVIER SAS

  公开号：WO2021155006A1

  公开（公告）日：2021-08-05

  Provided are novel compounds of Formula (I); pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by CDK such as cancer.

  提供了式（I）的新化合物；其药用盐，以及药物组合物，可用于治疗由CDK介导的癌症等疾病和疾病。
• Bismuth(III) Chloride Catalyzed Efficient and Selective Cleavage of Trityl Ethers
  作者：Gowravaram Sabitha、E. Venkata Reddy、R. Swapna、N. Mallikarjun Reddy、J. S. Yadav

  DOI：10.1055/s-2004-825602

  日期：——

  A highly selective and efficient protocol has been developed for detritylation using 5 mol% BiCl 3 in acetonitrile. The cleavage proceeds at room temperature in high yields and the conditions are mild enough to tolerate avariety of acid-base sensitive functional groups.

  已开发出一种使用 5 mol% BiCl 3 乙腈溶液进行脱三苯甲基化的高选择性和高效方案。裂解在室温下以高产率进行，条件温和到足以耐受各种酸碱敏感官能团。
• Identification and Development of Biphenyl Substituted Iminosugars as Improved Dual Glucosylceramide Synthase/Neutral Glucosylceramidase Inhibitors
  作者：Amar T. Ghisaidoobe、Richard J. B. H. N. van den Berg、Saleem S. Butt、Anneke Strijland、Wilma E. Donker-Koopman、Saskia Scheij、Adrianus M. C. H. van den Nieuwendijk、Gerrit-Jan Koomen、Arnold van Loevezijn、Mark Leemhuis、Tom Wennekes、Mario van der Stelt、Gijsbert A. van der Marel、Constant A. A. van Boeckel、Johannes M. F. G. Aerts、Herman S. Overkleeft

  DOI：10.1021/jm501181z

  日期：2014.11.13

  This work details the evaluation of a number of N-alkylated deoxynojirimycin derivatives on their merits as dual glucosylceramide synthase/neutral glucosylceramidase inhibitors. Building on our previous work, we synthesized a series of d-gluco and l-ido-configured iminosugars N-modified with a variety of hydrophobic functional groups. We found that iminosugars featuring N-pentyloxymethylaryl substituents are considerably more potent inhibitors of glucosylceramide synthase than their aliphatic counterparts. In a next optimization round, we explored a series of biphenyl-substituted iminosugars of both configurations (d-gluco and l-ido) with the aim to introduce structural features known to confer metabolic stability to drug-like molecules. From these series, two sets of molecules emerge as lead series for further profiling. Biphenyl-substituted l-ido-configured deoxynojirimycin derivatives are selective for glucosylceramidase and the nonlysosomal glucosylceramidase, and we consider these as leads for the treatment of neuropathological lysosomal storage disorders. Their d-gluco-counterparts are also potent inhibitors of intestinal glycosidases, and because of this characteristic, we regard these as the prime candidates for type 2 diabetes therapeutics.
• [EN] BIFUNCTIONAL COMPOUND USING UBR BOX DOMAIN-BINDING LIGAND<br/>[FR] COMPOSÉ BIFONCTIONNEL UTILISANT UN LIGAND LIANT LE DOMAINE DE BOÎTE UBR<br/>[KO] UBR 박스 도메인 결합 리간드를 이용한 이중기능성 화합물
  申请人：[en]AUTOTAC INC.;[ko]주식회사 오토텍바이오

  公开号：WO2023074936A1

  公开（公告）日：2023-05-04

  본 명세서에서 개시하는 내용은 UBR 박스 도메인 결합 리간드를 이용한 이중기능성(bifunctional) 화합물에 관한 것이다. 상기 UBR 박스 도메인은 N-말단 경로 법칙(N-end rule pathway)의 UBR(Ubiquitin protein ligase E3 component n-recognin)단백질 내에 공통적으로 존재하는 도메인이다. 이 때 상기 UBR 박스 도메인은 기질(substrate)이 결합하는 도메인으로 알려져 있다. 상기 UBR 박스 도메인은 기질의 N-말단 잔기에 결합하여 기질에 멀티 유비퀴틴 사슬을 형성하는데 필수적이며, 기질은 이 과정을 통해 분해된다고 알려져 있다. 이러한 UBR 박스 도메인의 기능을 이용하는 UBR 박스 도메인 리간드를 이용한 이중기능성(bifunctional) 화합물을 이용해 원하는 타겟 단백질(또는 펩타이드)을 보다 효과적으로 분해시키도록 유도할 수 있다.