N,N-二甲基苯甲酰胺二甲缩醛 | 35452-04-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N,N-二甲基苯甲酰胺二甲缩醛
• 英文名称: N,N-dimethylbenzamide dimethyl acetal
• 英文别名: 1,1-dimethoxy-N,N-dimethyl-1-phenylmethanamine
• CAS: 35452-04-1
• 化学式: C₁₁H₁₇NO₂
• 分子量: 195.261
• InChiKey: DLYZPQGVPVAEME-UHFFFAOYSA-N

物化性质

• 沸点：
  219℃
• 密度：
  1.013
• 闪点：
  60℃

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  21.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N,N-二甲基苯甲酰胺二甲缩醛 在 L-Selectride 作用下， 以 四氢呋喃 、 甲苯 为溶剂， 反应 1.0h， 生成 (E)-isopropyl 4-methoxy-2-phenyl-6-(prop-1-enyl)-5,6-dihydro-2H-pyran-3-carboxylate
  参考文献：
  名称：

  A Maitland–Japp inspired synthesis of dihydropyran-4-ones and their stereoselective conversion to functionalised tetrahydropyran-4-ones

  摘要：

  已开发出新的Maitland–Japp反应变体，可用于合成带有三级和四级立体中心的二氢吡喃和四氢吡喃，包括Civet中的官能化四氢吡喃和lasonolide A的A环。

  DOI：

  10.1039/c5ob00292c

文献信息

• Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat
  作者：Jay Wrobel、Jane Millen、Janet Sredy、Arlene Dietrich、Joseph M. Kelly、Beverly J. Gorham、Kazimir Sestanj

  DOI：10.1021/jm00131a012

  日期：1989.11

  A series of aldose reductase inhibitors was prepared in which structural modifications were made to three positions of the potent, orally active inhibitor tolrestat (1), namely, the 6-methoxy substituent, thioamide sulfur, and the N-methyl moiety. These compounds were evaluated in two in vitro systems: an isolated enzyme preparation from bovine lens to assess their intrinsic inhibitory activity and

  制备了一系列醛糖还原酶抑制剂，其中对有效的口服活性抑制剂托瑞司他（1）的三个位置进行了结构修饰，即6-甲氧基取代基，硫代酰胺硫和N-甲基部分。在两个体外系统中对这些化合物进行了评估：从牛晶状体分离的酶制剂以评估其固有的抑制活性，在大鼠的坐骨神经测定法中通过分离的大鼠坐骨神经测定以确定其穿透神经组织膜的能力。还对这些化合物作为半乳糖醇在半乳糖喂养大鼠的晶状体，坐骨神经和隔膜中蓄积的抑制剂进行了体内评估。用甲硫基取代基对1的6-甲氧基进行生物等位取代，得到5，用氰基idine取代1的硫酰胺取代基，得到7。5和7均保留了较高的体外效价，但在体内却不如1高效。用碳甲氧基取代了torerestat N-甲基，得到10，导致所用三种测定中的每一种均大大降低了活性。但是，对oxo-tolrestat（2）的相同结构修饰导致11，并导致内在活性增强和相当的体内效价。孤立的神经数据表明，这些化合物中的某些化
• Process for Preparing Sucrose-6-ester
  申请人：Wu Jing Jun

  公开号：US20080058508A1

  公开（公告）日：2008-03-06

  This invention relates to a method for preparing a sucrose-6-ester. The method includes (i) reacting sucrose with a N,N-dimethylcarboxamide dimethyl acetal in an inert aprotic solvent to form a cyclic acetal of formula (I): wherein R is C 1 -C 6 alkyl, C 3 -C 20 cycloalkyl, C 1 -C 20 heterocycloalkyl, aryl, or heteroaryl; and (ii) subjecting the cyclic acetal to a mild acidic or neutral hydrolysis to provide a sucrose-6-ester of formula (II):

  这项发明涉及一种制备蔗糖-6-酯的方法。该方法包括（i）将蔗糖与N,N-二甲基羧酰胺二甲基缩醛在惰性非质子溶剂中反应，形成式（I）的环缩醛：其中R为C1-C6烷基、C3-C20环烷基、C1-C20杂环烷基、芳基或杂芳基；以及（ii）将环缩醛暴露于温和酸性或中性水解条件下，得到式（II）的蔗糖-6-酯。
• Substituted pyrrole derivatives and their use as HMG-CO inhibitors
  申请人：Ranbaxy Laboratories Limited

  公开号：EP2319843A1

  公开（公告）日：2011-05-11

  The present invention relates to substituted pyrrole derivatives, which can be used as 2-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Compounds disclosed herein can function as cholesterol lowering agents and can be used for the treatment of cholesterol-related diseases and related symptoms. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and methods of treating cholesterol-related diseases and related symptoms.

  本发明涉及可用作 2-羟基-3-甲基戊二酰辅酶 A（HMG-CoA）还原酶抑制剂的取代吡咯衍生物。本文公开的化合物可作为降低胆固醇的药物，并可用于治疗胆固醇相关疾病及相关症状。本文提供了制备所公开化合物的工艺，以及含有所公开化合物的药物组合物和治疗胆固醇相关疾病及相关症状的方法。
• Nature of the slow step in the hydrolysis of cyclic and bicyclic ortho esters containing 1,3-dioxane rings
  作者：Robert A. McClelland、Sherrin Gedge、Jon Bohonek

  DOI：10.1021/jo00318a013

  日期：1981.2
• 1,3-Diaza-1,3-butadienes. Synthesis and Conversion into Pyrimidines by [4π + 2π] Cycloaddition with Electron Deficient Acetylenes. Synthetic Utility of 2-(Trichloromethyl)pyrimidines¹
  作者：Angel Guzmán、Moisés Romero、Francisco X. Talamás、Rene Villena、Robert Greenhouse、Joseph M. Muchowski

  DOI：10.1021/jo952106w

  日期：1996.1.1

  Methods have been devised to generate 1H-1,3-diaza-1,3-butadienes bearing a leaving group at position-4 in latent, masked, and unprotected forms. A hallmark of these azadienes is that they undergo thermal [4 pi + 2 pi] cycloaddition reactions with electron deficient acetylenes to give adducts which are aromatized to pyrimidine derivatives under the reaction conditions. Thus, 1-(methoxycarbonyl)-3-acylamidines 17 on beating in solution are converted in situ into the 1,3-diaza-1,3-dienes 18 and/or 19 which react with dimethyl acetylenedicarboxylate (DMAD) to produce the pyrimidines 20. The 1-Boc-1,3-diaza-1,3-dienes 24 are masked forms of the LH-dienes inasmuch as they react with DMAD under relatively mild conditions to give the dihydropyrimidine adducts 25, which are easily detectable by H-1 NMR spectroscopy, and which aromatize to pyrimidines 26 at higher temperatures. The 4-methylthio compounds 31 and 33, and the 2-(trichloromethyl) compounds 37, are isolable, relatively stable, 1H-1,3-diaza-1,3-butadienes, These easily prepared compounds react with electron deficient acetylenes under mild conditions to provide the pyrimidines 20, 34, and 38, respectively, in fair to excellent yields. The 2-(trichloromethyl)pyrimidines 38 are very useful precursors of a wide variety of other 2-substituted pyrimidines 46-52.