lithium,methanidylsulfonylmethane | 17609-14-2

• 分子结构分类: 有机化合物 - 有机硫化合物 - 磺酰类
• 英文名称: lithium,methanidylsulfonylmethane
• 英文别名: methylsulphonylmethyl-lithium；lithio methyl sulfone
• CAS: 17609-14-2
• 化学式: C₂H₅LiO₂S
• 分子量: 100.067
• InChiKey: VZYIGMUABYWRBG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.84
• 重原子数：
  6.0
• 可旋转键数：
  1.0
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  34.14
• 氢给体数：
  0.0
• 氢受体数：
  2.0

反应信息

• 作为反应物：
  描述：

  lithium,methanidylsulfonylmethane 、 ethyl 2-oxo-6-phenyl-1,2-dihydropyridine-3-carboxylate 生成 3-(2-Methanesulfonyl-acetyl)-6-phenyl-1H-pyridin-2-one
  参考文献：
  名称：

  McCombie, Stuart W.; Lin, Sue-Ing; Tagat, Jayaram R., Heterocycles, 1993, vol. 35, # 1, p. 93 - 97

  摘要：

  DOI：
• 作为产物：
  描述：

  二甲基砜 在 正丁基锂 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 0.25h， 生成 lithium,methanidylsulfonylmethane
  参考文献：
  名称：

  含有磺酰基稳定碳负离子作为不可转移配体的混合高碳酸酯的反应

  摘要：

  在四氢呋喃中先用碘化亚铜（I）处理α-石棉砜，然后用1 mol处理。当量 烷基锂或格氏试剂的混合物会产生混合的纯铜[R'SO 2 CH 2 CuR] – M +（M = Li或MgX），是将R共轭加成烯酮并将酰氯中的氯化物取代成R的有效试剂产生酮（收率> 90％）。

  DOI：

  10.1039/c39820000358

文献信息

• Ring Opening of Cyclic Vinylogous Acyl Triflates Using Stabilized Carbanion Nucleophiles: Claisen Condensation Linked to Carbon−Carbon Bond Cleavage
  作者：David M. Jones、Marilda P. Lisboa、Shin Kamijo、Gregory B. Dudley

  DOI：10.1021/jo100249g

  日期：2010.5.21

  Addition of stabilized carbanionic nucleophiles to cyclic vinylogous acyl triflates (VATs) triggers a ring-opening fragmentation to give acyclic β-keto ester and related products, much like those observed traditionally in the Claisen condensation. Unlike in the classical Claisen condensation, however, the VAT-Claisen reaction described herein is rendered irreversible by C−C bond cleavage, not by deprotonation

  在环状乙烯基乙烯基三氟甲磺酸酯（VAT）中添加稳定的碳负离子亲核试剂会触发开环断裂，生成无环β-酮酯和相关产物，就像传统上在克莱森缩合反应中观察到的那样。但是，与经典的克莱森缩合不同，本文所述的VAT-克莱森反应通过C-C键裂解而不是通过活化的亚甲基产物的去质子化而变得不可逆。本文公开了该原始反应方法的全部细节，包括各种亲核试剂之间的细微差异如何影响对制备1，3-二酮，β-酮酸酯和β-酮膦酸酯的反应条件的正确选择。
• 2-Amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
  申请人：Sher M. Philip

  公开号：US20060111338A1

  公开（公告）日：2006-05-25

  Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer. These novel compounds have the structure or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, R 1 , R 2 , X and Z are defined herein.

  提供了一些新的化合物，它们是糖原磷酸化酶抑制剂，可用于治疗、预防或减缓需要糖原磷酸化酶抑制剂治疗的疾病，如糖尿病及相关疾病（如高血糖、糖耐量受损、胰岛素抵抗和高胰岛素血症），与糖尿病相关的微血管并发症（如视网膜病变、神经病变、肾病和延迟伤口愈合），与糖尿病相关的大血管并发症（心血管疾病，如动脉粥样硬化、心脏功能异常、心肌缺血和中风），以及代谢综合征及其组成疾病，包括高血压、肥胖和脂质代谢异常（包括高三酸甘油酯血症、高胆固醇血症和低高密度脂蛋白血症），以及其他疾病，如非心脏缺血、感染和癌症。这些新的化合物具有特定的结构、立体异构体、前药或其药用可接受的盐，其中W、R1、R2、X和Z在此处有定义。
• HETEROARYL DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
  申请人：Zhejiang Hisun Pharmaceutical Co., Ltd.

  公开号：EP4092019A1

  公开（公告）日：2022-11-23

  The present invention relates to heteroaryl derivatives, preparation methods therefor, and applications thereof in medicine. Specifically, the present invention relates to a heteroaryl derivative represented by general formula (AI), a preparation method therefor, and a pharmaceutically acceptable salt, and use thereof as a therapeutic agent, in partucular, as an SHP2 allosteric inhibitor, wherein the definition of substituents in general formula (AI) is the same as that in the description.

  本发明涉及杂环芳基衍生物、其制备方法和在医学上的应用。具体地，本发明涉及一种由通式（AI）表示的杂环芳基衍生物、其制备方法、药学上可接受的盐以及作为治疗剂的用途，特别是作为SHP2变构抑制剂，其中通式（AI）中取代基的定义与描述中相同。
• Huby, Nicholas J. S.; Kinsman, Richard G.; Lathbury, David, Journal of the Chemical Society. Perkin transactions I, 1991, # 1, p. 145 - 155
  作者：Huby, Nicholas J. S.、Kinsman, Richard G.、Lathbury, David、Vernon, Peter G.、Gallagher, Timothy

  DOI：——

  日期：——
• The LiClO4-Mediated Synthesis of β-(Dialkylamino) Sulfoxides and β-(Dialkylamino) Sulfones by Addition of α-Lithiated Salts of Sulfoxides and Sulfones to Aldehydes and (Trimethylsilyl)dialkylamines
  作者：M. Reza Naimi-Jamal、Junes Ipaktschi、Mohammad R. Saidi

  DOI：10.1002/(sici)1099-0690(200005)2000:9<1735::aid-ejoc1735>3.0.co;2-a

  日期：2000.5

  The LiClO4-mediated one-pot reaction of aldehydes with (trimethylsilyl)dialkyl amines and the lithium salt of sulfoxides or sulfones, affords the corresponding beta-(dialkylamino) sulfoxides and beta-(dialkylamino) sulfones in high yields. The aminosulfoxidation reaction of aliphatic or aromatic aldehydes lacks diastereoselectivity, but the diastereomeric sulfoxides can be separated by HPLC or column chromatography for further use.