iodomethanesulfonyl chloride | 22354-05-8

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 磺酰卤
• 英文名称: iodomethanesulfonyl chloride
• 英文别名: Jod-methansulfonylchlorid；Jodmethansulfonsaeure-chlorid；iodomethane sulphonylchloride；Iodmethansulfonsaeure-chlorid；Iodmethansulfonylchlorid
• CAS: 22354-05-8
• 化学式: CH₂ClIO₂S
• mdl: MFCD19200093
• 分子量: 240.449
• InChiKey: HLVPPXHUMMLBLD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  6
• 可旋转键数：
  1
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  42.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  iodomethanesulfonyl chloride 在 氨 作用下， 生成 C-iodo-methanesulfonamide
  参考文献：
  名称：

  Binz; Maier-Bode, Biochemische Zeitschrift, 1932, vol. 252, p. 20

  摘要：

  DOI：
• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 氯仿 、 五氯化磷 作用下， 生成 iodomethanesulfonyl chloride
  参考文献：
  名称：

  Binz; Maier-Bode, Biochemische Zeitschrift, 1932, vol. 252, p. 20

  摘要：

  DOI：

文献信息

• Protocol for Stereoselective Construction of Highly Functionalized Dienyl Sulfonyl Fluoride Warheads
  作者：Zai-Wei Zhang、Shi-Meng Wang、Wan-Yin Fang、Ravindar Lekkala、Hua-Li Qin

  DOI：10.1021/acs.joc.0c01877

  日期：2020.11.6

  A pyrrolidine-mediated Knoevenagel-type reaction for highly stereoselective construction of novel α-halo-1,3-dienylsulfonyl fluorides was achieved in up to 100% Z-selectivity and high yields at room temperature from condensation of the readily available aldehydes and halomethanesulfonyl fluorides. This protocol provided a class of unique α-halo-1,3-dienylsulfonyl fluorides with wide scope and excellent

  吡咯烷介导的Knoevenagel型反应可实现高度立体选择性地构建新型α-卤代1,3,2-二烯基磺酰氟，在室温下通过易得的醛类和卤代甲磺酰氟的缩合可实现高达100％的Z选择性和高收率。 。该方案提供了一类独特的α-卤代-1,3-二烯基磺酰氟，具有宽范围和出色的官能团相容性。α-卤代1，，3-二烯基磺酰氟被用作氟化硫交换点击化学，Suzuki反应和Sonogashira反应中的通用构件，用于组装高度官能化的二烯基磺酰氟衍生物，用作共价战斗部以发现新药。
• [EN] C5-C6 OXACYCLIC-FUSED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE<br/>[FR] COMPOSÉS DE DIOXYDE DE THIADIAZINE CONDENSÉS AVEC DES DÉRIVÉS OXACYCLIQUES EN C5-C6 COMME INHIBITEURS DE BACE, COMPOSITIONS, ET UTILISATION USE
  申请人：MERCK SHARP & DOHME

  公开号：WO2012138734A1

  公开（公告）日：2012-10-11

  In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula : (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of ring A, ring B, ring C, R2, R3, R4, m, n, p, and -L1- is as defined herein. The novel compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.

  在其许多实施方式中，本发明提供了某些咪唑噻二唑二氧化物化合物，包括化合物式：(I)及其互变异构体和立体异构体，以及该化合物的药用可接受盐，所述互变异构体和所述立体异构体，其中环A、环B、环C、R2、R3、R4、m、n、p和-L1-的定义如本文所述。本发明的新化合物可能有助于作为BACE抑制剂和/或用于治疗和预防与之相关的各种病理病变。还公开了包括一个或多个此类化合物的制药组合物（单独或与一个或多个其他活性剂的组合），以及其制备和使用方法，包括治疗阿尔茨海默病。
• Synthesis and use of sulfonamide-, sulfoxide-, or sulfone-containing aminoglycoside–CoA bisubstrates as mechanistic probes for aminoglycoside N-6′-acetyltransferase
  作者：Feng Gao、Xuxu Yan、Omar Zahr、Aaron Larsen、Kenward Vong、Karine Auclair

  DOI：10.1016/j.bmcl.2008.09.004

  日期：2008.10

  Aminoglycoside-coenzyme A conjugates are challenging synthetic targets because of the wealth of functional groups and high polarity of the starting materials. We previously reported a one-pot synthesis of amide-linked aminoglycoside-CoA bisubstrates. These molecules are nanomolar inhibitors of aminoglycoside N-6'-acetyltransferase Ii (AAC(6')-Ii), an important enzyme involved in bacterial resistance

  氨基糖苷-辅酶A共轭物因具有丰富的官能团和起始原料的高极性而成为具有挑战性的合成靶标。我们以前报道过一锅法合成酰胺连接的氨基糖苷-CoA双底物。这些分子是氨基糖苷N-6'-乙酰基转移酶Ii（AAC（6'）-Ii）的纳摩尔抑制剂，这是一种对细菌对氨基糖苷抗生素具有抗性的重要酶。我们在这里报告了五个新的包含磺酰胺，亚砜或砜基团的氨基糖苷-CoA双底物的合成和生物活性。有趣的是，与酰胺连接的双底物相比，预期最能模仿四面体中间体的磺酰胺连接的双底物没有显示出改善的抑制作用。另一方面，
• Amido derivatives of 2,4,6-triiodobenzoic acids containing at least one
  申请人：Nyegaard & Co. A/S

  公开号：US04021481A1

  公开（公告）日：1977-05-03

  This invention relates to novel X-ray contrast agents particularly for use in the cerebrospinal cavities, comprising non-ionic alkanols carrying at least one N-bonded secondary or tertiary amide group and having at least two hydroxyl groups and at least one iodine atom in the molecule. Particularly useful compounds include the N-hydroxyalkyl iodoalkane sulphonamides having at least two hydroxyl groups, tri- and tetra-iodobenzene carrying carbamoyl, acylamino and/or acylaminomethyl substituents and having at least two hydroxyl groups in the molecule and at least one N-hydroxyalkyl group. Particularly preferred compounds comprise 2,4,6-triiodobenzamides which may be 3- and/or 5-substituted with a variety of groups. The compounds all show markedly low toxicities and a number show very high levels of water solubility.

  这项发明涉及新型X射线造影剂，特别用于脑脊液腔，包括携带至少一个N-键合的二次或三次酰胺基团并且分子中至少有两个羟基和至少一个碘原子的非离子烷醇。特别有用的化合物包括至少有两个羟基的N-羟基烷基碘烷磺酰胺，携带氨基甲酰、酰胺基或酰氨基甲基取代基并且分子中至少有两个羟基和至少一个N-羟基的三碘苯和四碘苯。特别优选的化合物包括2,4,6-三碘苯酰胺，它们可能在3-和/或5-位置上被各种基团取代。这些化合物都表现出明显低的毒性，其中一些化合物具有非常高的水溶性水平。
• 2-Haloethylating agents for cancer chemotherapy. 2-Haloethyl sulfonates
  作者：Y. Fulmer Shealy、Charles A. Krauth、Robert F. Struck、John A. Montgomery

  DOI：10.1021/jm00362a016

  日期：1983.8

  Because certain (2-chloroethyl)triazenes and (2-haloethyl)nitrosoureas have high antineoplastic activity, 2-chloroethyl and 2-fluoroethyl sulfonates were prepared to try to develop additional types of 2-haloethylating agents. In this initial study, it was demonstrated that antineoplastic activity much superior to that of the prototype, 2-chloroethyl methanesulfonate, could be found among 2-chloroethyl

  由于某些（2-氯乙基）三氮烯和（2-卤乙基）亚硝基脲具有很高的抗肿瘤活性，因此准备了2-氯乙基和2-氟乙基磺酸盐以尝试开发其他类型的2-卤乙基化剂。在这项初步研究中，证明了在2-氯乙基磺酸盐中可以发现抗肿瘤活性大大优于原型2-氯乙基甲烷磺酸盐。在各种2-氯乙基烷烃和芳烃磺酸盐中，几种取代的甲磺酸盐对小鼠的P388白血病表现出显着的活性。氯甲烷磺酸盐显示出高活性（T / C = 218％）。该测试中没有任何一种芳烃磺酸盐。