SYNTHESIS OF N,N-DIALKYL, -DIALKENYL, -DIALKYNL, AND RELATED CYCLICS, SULFAMOYL FLUORIDE COMPOUNDS USING HYDROGEN FLUORIDE
摘要:
Methods of producing N,N-dimethyl sulfamoyl fluoride and related derivatives of the formula F—S(O)2—NR2(I) by contacting a sulfamoyl nonfluorohalide compound of the formula X—S(O)2—NR2(II) with anhydrous hydrogen fluoride under conditions sufficient to produce the N,N-dimethyl sulfamoyl fluoride or derivative thereof of Formula I, wherein R in each of Formulas I and II is, independently, a linear or branched alkyl, alkenyl, or alkynyl group containing 1 to 12 carbon atoms, the Rs can be joined to form a cyclic amine with the N, and X is any one of chlorine, bromine, and iodine.
[EN] CONDENSED THIOPHENE DERIVATIVES USEFUL AS NAPI-IIB INHIBITORS<br/>[FR] DÉRIVÉS DE THIOPHÈNE CONDENSÉS UTILES EN TANT QU'INHIBITEURS DE NAPI-IIB
申请人:LILLY CO ELI
公开号:WO2018034883A1
公开(公告)日:2018-02-22
The invention provides compounds of the formula: (A), pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using these compounds, salts, or compositions to treat hyperphosphatemia, chronic kidney disease, and/or the cardiovascular diease associated with chronic kidney disease.
[EN] N-METHYL-N-(1-PHENYL-2-(1-PYRROLIDINYL)ETHYL)-2-AMINOPHENYLACETAMIDE DERIVATIVES AGONISTS FOR THE KAPPA OPIOID RECEPTOR<br/>[FR] AGONISTES DE DÉRIVÉS N-MÉTHYL-N-(1-PHÉNYL-2-(1-PYRROLIDINYL)ÉTHYL)-2-AMINOPHÉNYLACÉTAMIDE POUR LE RÉCEPTEUR OPIOÏDE KAPPA
申请人:NEKTAR THERAPEUTICS
公开号:WO2016106133A1
公开(公告)日:2016-06-30
Compounds and pharmaceutically acceptable salts and solvates thereof are described. The compounds relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology and organic chemistry.
Silyl Radical-Mediated Activation of Sulfamoyl Chlorides Enables Direct Access to Aliphatic Sulfonamides from Alkenes
作者:Sandrine M. Hell、Claudio F. Meyer、Gabriele Laudadio、Antonio Misale、Michael C. Willis、Timothy Noël、Andrés A. Trabanco、Véronique Gouverneur
DOI:10.1021/jacs.9b13071
日期:2020.1.15
However, sulfamoyl and sulfonyl chlorides can be easily activated by Cl-atom abstrac-tion by a silyl radical with similar rates. This later mode of acti-vation was therefore selected to access aliphatic sulfonamides applying a single-step hydrosulfamoylation using inexpensive olefins, tris(trimethylsilyl)silane and photocatalyst Eosin Y. This late-stage functionalization protocol generates molecules
氨磺酰氯的单电子还原比磺酰氯更具挑战性。然而,氨磺酰氯和磺酰氯可以很容易地通过甲硅烷基的 Cl 原子提取以相似的速率被激活。因此,选择这种后期的活化模式来获得脂肪族磺酰胺,使用廉价的烯烃、三(三甲基甲硅烷基)硅烷和光催化剂曙红 Y 进行单步氢氨磺酰化。这种后期功能化方案生成的分子与含磺酰胺的环丁基-直接用于药物化学的螺环吲哚。
Photocatalyst-Free Activation of Sulfamoyl Chlorides for Regioselective Sulfamoyl-Oximation of Alkenes via Hydrogen Atom Transfer (HAT) and Halogen-Atom Transfer (XAT) Relay Strategy
作者:Wei Li、Zhihua Huang、Deliang Zhong、Huaifeng Li
DOI:10.1021/acs.orglett.4c00314
日期:2024.3.15
methodologies have been limited to either the use of photocatalyst or the monofunctionalization of activated alkenes. Here, we report a regioselective sulfamoyl-oximation of alkenes by involving the activation of sulfamoyl chlorides through a HAT and XAT relay strategy in a photocatalyst-free way. The key to this success lies in the dual roles of tert-butyl nitrite (TBN), which not only serves as the source
使用容易获得的多种氨磺酰氯来合成磺酰胺化合物是一种有趣但尚未充分探索的策略。由于氨磺酰氯的高还原电位,通过单电子还原激活氨磺酰氯面临着挑战。或者,氨磺酰氯中的SO 2 –Cl 键很容易被XAT 裂解。然而,现有的方法仅限于使用光催化剂或活化烯烃的单官能化。在这里,我们报道了烯烃的区域选择性氨磺酰肟化,通过 HAT 和 XAT 中继策略以无光催化剂的方式激活氨磺酰氯。这一成功的关键在于亚硝酸叔丁酯 (TBN) 的双重作用,它不仅充当肟的来源,还充当 HAT 试剂来生成关键的 XAT 反应物种。排除利用光能的金属催化剂或光敏剂使得该协议具有通用性并且普遍适用于合成各种结构多样的含肟的烷基磺酰胺。
N-methyl-N-(1-phenyl-2-(1-pyrrolidinyl)ethyl)-2-aminophenylacetamide derivatives agonists for the kappa opioid receptor
申请人:Nektar Therapeutics
公开号:US10322107B2
公开(公告)日:2019-06-18
Compounds and pharmaceutically acceptable salts and solvates thereof are described. The compounds relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology and organic chemistry.