- Regioselective Bromine/Magnesium Exchange for the Selective Functionalization of Polyhalogenated Arenes and Heterocycles
-
Using the bimetallic combination sBu2Mg?2 LiOR (R=2-ethylhexyl) in toluene enables efficient and regioselective Br/Mg exchanges with various dibromo-arenes and -heteroarenes under mild reaction conditions and provides bromo-substituted magnesiu
- Desaintjean, Alexandre,Haupt, Tobias,Bole, Leonie J.,Judge, Neil R.,Hevia, Eva,Knochel, Paul
-
supporting information
p. 1513 - 1518
(2020/11/30)
-
- Disposable cartridge concept for the on-demand synthesis of turbo Grignards, Knochel–Hauser amides, and magnesium alkoxides
-
Magnesium organometallic reagents occupy a central position in organic synthesis. The freshness of these compounds is the key for achieving a high conversion and reproducible results. Common methods for the synthesis of Grignard reagents from metallic magnesium present safety issues and exhibit a batch-to-batch variability. Tubular reactors of solid reagents combined with solution-phase reagents enable the continuous-flow preparation of organomagnesium reagents. The use of stratified packed-bed columns of magnesium metal and lithium chloride for the synthesis of highly concentrated turbo Grignards is reported. A low-cost pod-style synthesizer prototype, which incorporates single-use prepacked perfluorinated cartridges and bags of reagents for the automated on-demand lab-scale synthesis of carbon, nitrogen, and oxygen turbo magnesium bases is presented. This concept will provide access to fresh organomagnesium reagents on a discovery scale and will do so independent from the operator’s experience in flow and/or organometallic chemistry.
- Adamo, Andrea,Berton, Mateo,McQuade, D. Tyler,Sheehan, Kevin
-
supporting information
p. 1343 - 1356
(2020/07/10)
-
- Nitrile-substituted 2-(oxazolinyl)-phenols: Minimalistic excited-state intramolecular proton transfer (ESIPT)-based fluorophores
-
Herein, we present minimalistic single-benzene, excited-state intramolecular proton transfer (ESIPT)-based fluorophores as powerful solid-state emitters. The very simple synthesis gave access to all four regioisomers of nitrile-substituted 2-(oxazolinyl)-
- Duvinage, Daniel,G?bel, Dominik,Nachtsheim, Boris J.,Stauch, Tim
-
supporting information
p. 9213 - 9225
(2020/07/27)
-
- Emission color-tunable oxazol(in)yl-substituted excited-state intramolecular proton transfer (ESIPT)-based luminophores
-
Oxazolinyl- and arylchalcogenazolyl-substituted hydroxyfluorenes exhibiting excited-state intramolecular proton transfer (ESIPT) are described as potent and highly modular luminophores. Emission color tuning was achieved by varying the π-expansion and the
- Bigall, Nadja C.,Duvinage, Daniel,G?bel, Dominik,Nachtsheim, Boris J.,Rusch, Pascal
-
supporting information
p. 15430 - 15433
(2020/12/25)
-
- Thiolation of Pyridine-2-sulfonamides using Magnesium Thiolates
-
The thiolation of pyridine-2-sulfonamides using magnesium thiolates is reported. The ortho-functionalizations of these sulfonamides using TMPMgCl·LiCl (TMP = 2,2,6,6-tetramethylpiperidyl) followed by electrophilic quenching produced a range of 3-functiona
- Balkenhohl, Moritz,Heinz, Benjamin,Knochel, Paul
-
p. 4452 - 4462
(2019/11/21)
-
- Zincation and Magnesiation of Functionalized Silylated Cyanohydrins Using TMP-Bases
-
Polyfunctional silylated cyanohydrins are readily magnesiated or zincated with TMPMgCl·LiCl or TMP 2 Zn·2MgCl 2 ·2LiCl leading to the corresponding metallated derivatives. These Mg- or Zn-derivatives react with various electrophiles such as benzylic bromides, allylic bromides, acid chlorides, aldehydes, NCCO 2 Et, or MeSO 2 SMe. Subsequently, TBAF-deprotection provides the corresponding keto or 1,2-diketo derivatives.
- Castelló-Micó, Alicia,Knochel, Paul
-
p. 155 - 169
(2017/10/07)
-
- NOVEL BRONCHODILATING DIAZAHETEROARYLS
-
The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
- -
-
Page/Page column 117
(2010/09/17)
-
- HETEROCYCLIC ANTIVIRAL COMPOUNDS
-
Compounds of formula I, wherein R1, R2, R3, X1, X2 and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
- -
-
Page/Page column 26
(2009/07/17)
-
- Non-nucleoside reverse transcriptase inhibitors
-
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
- -
-
Page/Page column 24
(2008/06/13)
-
- Heterocyclic antiviral compounds
-
The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.
- -
-
Page/Page column 21
(2010/02/15)
-
- Heterocyclic reverse transcriptase inhibitors
-
The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where R1, R2 and R3, are as defined herein.
- -
-
Page/Page column 9
(2010/11/24)
-
- Method of preparing organomagnesium compounds
-
The present invention is directed to a reagent for use in the preparation of organomagnesium compounds as well as to a method of preparing such organomagnesium compounds. The present invention furthermore provides a method of preparing functionalized or unfunctionalized organic compounds as well as the use of the reagents of the present invention in the preparation of organometallic compounds and their reaction with electrophiles. Finally, the present invention is directed to the use of lithium salts - LiY in the preparation of organometallic compounds and their reactions with electrophiles and to an organometallic compound which is obtainable by the disclosed method.
- -
-
Page/Page column 10
(2010/02/14)
-