2-(trimethylsilyl)ethoxymethoxy chloride

• 分子结构分类: 有机化合物 - 有机金属化合物 - 有机类金属化合物
• 英文名称: 2-(trimethylsilyl)ethoxymethoxy chloride
• 英文别名: chloro-(2-trimethylsilyl)ethoxymethane；chloromethyl 2-(trimethylsilyloxy)ethyl ether；2-(trimethylsilyloxy)ethoxymethyl chloride；2'-trimethylsilyloxyethoxymethyl chloride；Trimethylsiloxyethoxymethyl chloride；Chloromethyl 2-(trimethylsilyloxy)-1-ethyl ether；2-(chloromethoxy)ethoxy-trimethylsilane
• 化学式: C₆H₁₅ClO₂Si
• 分子量: 182.722
• InChiKey: WNNPBWBWGGUFLT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.05
• 重原子数：
  10
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  18.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(trimethylsilyl)ethoxymethoxy chloride 在 palladium on activated charcoal N-甲基吗啉 、 4-二甲氨基吡啶 、 氢气 、 双(2-氧代-3-恶唑烷基)次磷酰氯 、 氯甲酸异丙酯 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 乙酸乙酯 为溶剂， 生成 3-[2-({1-[6-benzyloxycarbonylamino-2-(2,2,2-trichloro-ethoxycarbonylamino)-hexanoyl]-pyrrolidine-2-carbonyl}-methyl-amino)-3-(4-methoxy-phenyl)-propionyloxy]-2-tert-butoxycarbonylamino-butyric acid 2-trimethylsilanyloxy-ethoxymethyl ester
  参考文献：
  名称：

  [Lys3]didemnins as potential affinity ligands

  摘要：

  The synthesis and biological activity of N-epsilon-Z-[Lys(3)]didemnin B are reported. This novel analogue retains antiproliferative, cytotoxic, and protein biosynthesis inhibition activities, but at reduced levels. This result suggests the use of [Lys(3)]didemnin derivatives as potential affinity probes for studying the molecular target(s) of the didemnin class of natural products. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00585-0

文献信息

• Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof
  申请人：Merck & Co., Inc.

  公开号：US06642237B1

  公开（公告）日：2003-11-04

  &ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

  -Hydroxy-2-(氟烷基氨基甲酰)-1-哌嗪戊二酰胺化合物是HIV蛋白酶的抑制剂，也是HIV复制的抑制剂。这些化合物在预防或治疗HV感染以及治疗艾滋病方面非常有用，无论是作为化合物、药学上可接受的盐、药物组成成分，还是与其他抗病毒药物、免疫调节剂、抗生素或疫苗组合使用。还描述了治疗艾滋病的方法以及预防或治疗HIV感染的方法。这些化合物对目前用于治疗艾滋病和HIV感染的HIV蛋白酶抑制剂产生耐药性的HIV病毒突变体具有有效作用。
• Synthesis of some C-8-modified 3-deoxy-β-d-manno-2-octulosonic acid analogs as inhibitors of CMP-Kdo synthetase
  作者：Jack Tadanier、Cheuk-Man Lee、David Whittern、Norman Wideburg

  DOI：10.1016/0008-6215(90)84236-n

  日期：1990.7

  Selective C-8 modifications of 2,6-anhydro-3-deoxy-D-glycero-D-talo-octonic acid ("2,3-dideoxy-beta-D-manno-2-octulosonic acid", 1a) were effected via the protected 8-hydroxy derivatives 2d and 2e. Swern oxidation of 2d and 2e gave the aldehydes 3a and 3b, respectively. Compounds 3a and 3b were converted into the oxime 13b and the O-methyloxime 13c derivatives, respectively. Methodology was developed

  对2,6-脱水-3-脱氧-D-甘油-D-talo-辛酸（“ 2,3-二脱氧-β-D-甘露-2-酸”，1a）进行了选择性的C-8修饰通过受保护的8-羟基衍生物2d和2e。2d和2e的Swern氧化分别得到醛3a和3b。将化合物3a和3b分别转化为肟13b和O-甲基肟13c衍生物。开发了选择性裂解13b和13c保护基以分别得到脱保护的肟12m和脱保护的O-甲基肟12n的方法。使用维蒂希方法从醛3a制备侧链增长的产品。从3a依次制备支链烯丙基胺12p，其关键步骤是使用LiCuMe2制备甲基酮19a，然后进行Swern氧化，使用CH 2 I 2 -Zn-TiCl 4对19a进行亚甲基化，得到烯烃19b，随后对19b进行Wohl-Ziegler溴化，得到烯丙基溴化物19c，并将后者转化为烯丙基叠氮化物19d。与CMP-Kdo合成酶相比，许多类似物显示出显着的活性。其中最活跃的是侧链延伸烯烃12d，其活性仅次于9-氨基类似物（1c）。
• [EN] NOVEL DIAZEPINE COMPOUNDS AS LIGANDS OF THE MELANOCORTIN 1 AND/OR 4 RECEPTORS<br/>[FR] NOUVEAUX COMPOSES DE DIAZEPINE UTILISES COMME LIGANDS DES RECEPTEURS 1 ET/OU 4 DE LA MELANOCORTINE
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2005118573A1

  公开（公告）日：2005-12-15

  There is provided novel diazepines that function as agonists at the melanocortin 4 receptor and as agonists at the melanocortin 1 receptor, pharmaceutical compositions containing them, methods for their use in treatment, and processes for their preparation.

  提供了一种新型的二氮杂环己烯类化合物，其在黑色素皮质素4受体上具有激动剂作用，并在黑色素皮质素1受体上也具有激动剂作用，包含它们的药物组合物，以及它们在治疗中的使用方法和制备过程。
• Oxamic acids and derivatives as thyroid receptor ligands
  申请人：Pfizer Inc.

  公开号：US06326398B1

  公开（公告）日：2001-12-04

  The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.

  本发明提供了Formula的新化合物及其前药，其几何和光学异构体，以及这些化合物、前药和异构体的药用可接受的盐，其中R1-R8和W如本文所述。还提供了含有这些化合物、前药、异构体或其药用可接受的盐的药物组合物，以及用于治疗肥胖、高脂血症、青光眼、心律失常、皮肤疾病、甲状腺疾病、甲状腺功能减退症和相关疾病如糖尿病、动脉粥样硬化、高血压、冠心病、高胆固醇血症、抑郁症和骨质疏松症的方法、药物组合物和工具包。
• Stereocontrolled synthesis of 2,4,5-trisubstituted tetrahydropyrans
  作者：Eiman H. Al-Mutairi、Stuart R. Crosby、Julia Darzi、Rachael A. Hughes、Thomas J. Simpson、Robert W. Smith、Christine L. Willis、John R. Harding、Clare D. King

  DOI：10.1039/b101414p

  日期：——

  Cyclisation of homoallylic acetals under acidic conditions leads to the formation of 2,4,5-trisubstituted tetrahydropyrans with the creation of two new asymmetric centres with excellent stereocontrol. By varying the acid and the nucleophile, the reaction may be adapted for the preparation of 2,4,5-trisubstituted tetrahydropyrans with either a halide, alcohol, acetate or amide at C-4.

  在酸性条件下高烯丙基缩醛的环化导致形成 2,4,5-三取代四氢吡喃，并产生两个具有出色立体控制的新不对称中心。通过改变酸和亲核试剂，该反应可适用于在 C-4 处用卤化物、醇、乙酸盐或酰胺制备 2,4,5-三取代四氢吡喃。