4-(tert-butyldimethylsilyloxy)-N-methylaniline | 90446-71-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-(tert-butyldimethylsilyloxy)-N-methylaniline
• 英文别名: 4-((tert-butyldimethylsilyl)oxy)-N-methylaniline；4-[tert-butyl(dimethyl)silyl]oxy-N-methylaniline
• CAS: 90446-71-2
• 化学式: C₁₃H₂₃NOSi
• 分子量: 237.417
• InChiKey: LOAOVMMNAPDXOT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.11
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(tert-butyldimethylsilyloxy)-N-methylaniline 在 四丁基氟化铵 、 三乙胺 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 反应 19.0h， 生成 N-(4-羟基苯基)-N-甲基苯甲酰胺
  参考文献：
  名称：

  Synthesis of new polyoxin derivatives and their activity against chitin synthase from Candida albicans

  摘要：

  Two analogues of L-alanylpolyoxin C with a modified peptide bond were synthesized and tested for inhibition of chitin synthase in Candida albicans. N-Methylation of the peptide bond (compound 13) or the replacement of it by NH2CH2 (compound 9) led to loss of activity in the enzyme assay. A novel analogue (compound 5) of nikkomycin was synthesized from uracil polyoxin C and (2S,3R)-3-hydroxyhomotyrosine, a component of echinocandin C. Despite high activity in the chitin synthase assay, 5 had no inhibitory effect on cells of C. albicans.

  DOI：

  10.1021/jm00381a003
• 作为产物：
  描述：

  N-甲基-P-氨基苯甲醚 在 咪唑 、 氢溴酸 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 11.0h， 生成 4-(tert-butyldimethylsilyloxy)-N-methylaniline
  参考文献：
  名称：

  Synthesis of new polyoxin derivatives and their activity against chitin synthase from Candida albicans

  摘要：

  Two analogues of L-alanylpolyoxin C with a modified peptide bond were synthesized and tested for inhibition of chitin synthase in Candida albicans. N-Methylation of the peptide bond (compound 13) or the replacement of it by NH2CH2 (compound 9) led to loss of activity in the enzyme assay. A novel analogue (compound 5) of nikkomycin was synthesized from uracil polyoxin C and (2S,3R)-3-hydroxyhomotyrosine, a component of echinocandin C. Despite high activity in the chitin synthase assay, 5 had no inhibitory effect on cells of C. albicans.

  DOI：

  10.1021/jm00381a003

文献信息

• [EN] NEW ISOINDOLINE OR ISOQUINOLINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] NOUVEAUX COMPOSÉS ISOINDOLINE OU ISOQUINOLÉINE, PROCÉDÉ POUR LEUR PRÉPARATION ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：SERVIER LAB

  公开号：WO2015011164A1

  公开（公告）日：2015-01-29

  Compounds of formula (I): (I) wherein Het, R3, R4, R5, R7, R8, R9, T, p, p', q, and q' are as defined in the description are pro-apoptotic agents useful in the treatment of cancers and of auto-immune and immune system diseases.

  式(I)的化合物：其中Het、R3、R4、R5、R7、R8、R9、T、p、p'、q和q'的定义如描述中所定义，是在治疗癌症以及自身免疫和免疫系统疾病中有用的促凋亡剂。
• REAGENTS FOR FLUOROSULFATING ALCOHOLS OR AMINES
  申请人：BIODURO, LLC

  公开号：US20190047950A1

  公开（公告）日：2019-02-14

  Disclosed herein are compounds of formula Ar—N(SO 2 F) 2 , wherein Ar is selected from an optionally substituted aryl, an optionally substituted five-membered heteroaryl, or an optionally substituted six-membered heteroaryl. Also disclosed are methods of synthesizing the above compounds by reacting a compound of formula Ar—NH—R 9 with MN(SO 2 F) 2 .

  本文披露了公式Ar—N(SO2F)2的化合物，其中Ar选自可选择取代的芳基、可选择取代的五元杂芳基或可选择取代的六元杂芳基。还披露了通过将公式Ar—NH—R9的化合物与MN(SO2F)2反应来合成上述化合物的方法。
• Introduction of a Crystalline, Shelf-Stable Reagent for the Synthesis of Sulfur(VI) Fluorides
  作者：Hua Zhou、Paramita Mukherjee、Rongqiang Liu、Edelweiss Evrard、Dianpeng Wang、John M. Humphrey、Todd W. Butler、Lise R. Hoth、Jeffrey B. Sperry、Sylvie K. Sakata、Christopher J. Helal、Christopher W. am Ende

  DOI：10.1021/acs.orglett.7b03950

  日期：2018.2.2

  The design, synthesis, and application of [4-(acetylamino)phenyl]imidodisulfuryl difluoride (AISF), a shelf-stable, crystalline reagent for the synthesis of sulfur(VI) fluorides, is described. The utility of AISF is demonstrated in the synthesis of a diverse array of aryl fluorosulfates and sulfamoyl fluorides under mild conditions. Additionally, a single-step preparation of AISF was developed that

  描述了[4-（乙酰氨基）苯基]亚氨基二硫基二氟化物（AISF）的设计，合成和应用，AISF是一种耐贮存的合成硫（VI）氟化物的结晶试剂。AISF的效用在温和条件下合成了多种芳基氟硫酸盐和氨磺酰氟得到了证明。此外，开发了AISF的单步制备方法，该方法利用氧化的C–H官能化方案将双（氟磺酰基）酰亚胺基团安装在乙酰苯胺上。
• 一种次氯酸荧光探针及其制备方法
  申请人：广东工业大学

  公开号：CN110016009B

  公开（公告）日：2021-05-11

  本发明涉及荧光探针技术领域，尤其涉及一种次氯酸荧光探针及其制备方法。本发明提供了一种次氯酸荧光探针，其分子式为C20H19NO2S，其结构式如式I所示。本发明还提供了上述次氯酸荧光探针的制备方法，分别通过偶联反应、取代反应和加成反应得到了次氯酸荧光探针。本发明提供的一种次氯酸荧光探针及其制备方法解决了现有的荧光探针灵敏度低、选择性差且成像应用有限的技术问题。
• ISOINDOLINE OR ISOQUINOLINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：LES LABORATOIRES SERVIER

  公开号：US20160194304A1

  公开（公告）日：2016-07-07

  Compounds of formula (I): wherein Het, R 3 , R 4 , R 5 , R 7 , R 8 , R 9 , T, p, p′, q, and q′ are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

  式(I)的化合物：其中，Het、R3、R4、R5、R7、R8、R9、T、p、p'、q和q'的定义如说明书所述。包含这些化合物的药物制剂在治疗涉及凋亡缺陷的病理学方面有用，例如癌症、自身免疫性疾病和免疫系统疾病。