- PROCESS FOR PREPARATION OF OPTICALLY ENRICHED ISOXAZOLINES
-
The invention relates to a process for preparing optically enriched isoxazoline compounds of formula (I), formula (I), wherein the variables are as defined in the specification, and the shown enantiomer has at least 55% ee; by oxo-Michael addition of hydr
- -
-
Page/Page column 12
(2021/10/11)
-
- NEW COMPOUNDS AND USES THEREOF FOR DETECTION OF TARGET MOLECULES IN A SAMPLE
-
The present invention relates to new profluorophores and conjugates thereof and their use for the detection of target molecule in a sample, in particular nucleic acid target molecules. The invention relates to new profluorophores and new fluorophores and methods of use thereof particularly useful in the fields of diagnostics and quality control.
- -
-
-
- Spin-Center Shift-Enabled Direct Enantioselective α-Benzylation of Aldehydes with Alcohols
-
Nature routinely engages alcohols as leaving groups, as DNA biosynthesis relies on the removal of water from ribonucleoside diphosphates by a radical-mediated "spin-center shift" (SCS) mechanism. Alcohols, however, remain underused as alkylating agents in synthetic chemistry due to their low reactivity in two-electron pathways. We report herein an enantioselective α-benzylation of aldehydes using alcohols as alkylating agents based on the mechanistic principle of spin-center shift. This strategy harnesses the dual activation modes of photoredox and organocatalysis, engaging the alcohol by SCS and capturing the resulting benzylic radical with a catalytically generated enamine. Mechanistic studies provide evidence for SCS as a key elementary step, identify the origins of competing reactions, and enable improvements in chemoselectivity by rational photocatalyst design.
- Nacsa, Eric D.,MacMillan, David W. C.
-
supporting information
p. 3322 - 3330
(2018/03/13)
-
- Anti-inflammatory agents
-
Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.
- -
-
-
- Selective photosensitization through an and logic response: Optimization of the pH and glutathione response of activatable photosensitizers
-
A series of pH and GSH responsive photosensitizers were designed and synthesized. pKa values were optimized by adjusting the inductive contribution of substituents to reach a pH range (6.0-7.4) relevant to the tumour microenvironment. pH-Activatable behaviour and redox mediated release of the quencher from the PS by GSH allow the construction of an AND logic operator for selective photodynamic action in aqueous solutions.
- Erbas-Cakmak, Sundus,Cakmak, Fatma Pir,Topel, Seda Demirel,Uyar, Taha Bilal,Akkaya, Engin U.
-
p. 12258 - 12261
(2015/07/27)
-
- TREATMENT OF DISEASES BY EPIGENETIC REGULATION
-
The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.
- -
-
-
- Hydroxymethylation and carbamoylation of di- and tetramethylpyridines using radical substitution (minisci) reactions
-
Reaction of hydroxymethyl radicals with N-methoxy 2,4- and 2,6- dimethylpyridinium salts gave 2,4,6-substituted hydroxymethylpyridines. Similar reactions with 2,3,5,6-tetramethylpyridine and derivatives failed, however 4-substitution could be achieved using a carbamoyl radical.
- Amrollahi Biyouki, Mohammad A.,Smith, Robin A. J.,Bedford, Jennifer J.,Leader, John P.
-
p. 3817 - 3825
(2007/10/03)
-
- AN IMPROVED METHOD FOR THE MONO-HYDROXYMETHYLATION OF PYRIDINES. A MODIFICATION OF THE MINISCI PROCEDURE
-
The reaction of N-methoxy-derivatives of pyridines in methanol with ammonium persulphate gives improved yields of mono-hydroxymethylated products.In contrast to the original Minisci procedure the reaction requires only catalytic amounts of ammonium persulphate.Evidence is presented which establishes that the reaction does not proceed via an intramolecular pathway.
- Katz, R B,Mistry, J,Mitchell, M B
-
p. 317 - 326
(2007/10/02)
-
- Nucleophilic Substitution in Quaternary Salts of NN'-Linked Biazoles and Related Systems.
-
Some reactions of dicationic and monocationic N,N'-linked biazoles and of quaternized 1-(N-azolyl)pyridinium ions with nucleophiles have been studied.Although the pyrrolyl nucleus has been found to be a poor leaving group in these reactions, in other cases nucleophilic attack readily takes place at an azolyl carbon atom, with subsequent elimination of the N-substituent.The 1-methyl-3-(1-methyl-1,2,4-triazol-4-ylio)benzimidazolium dication (1) reacted at room temperature with ammonium, diethylamine, methoxyde, hydroxide, and cyanide ions, and with sodium borohydride, giving in all cases the corresponding 2-substituted benzimidazoles in good yield.In the case of the 2,4,6-trimethyl-1-(2-methylpyrazol-1-io)pyridinium dication (6), the reaction with cyanide ion afforded, regioselectively, 5-cyano-1-methylpyrazole, with no trace of the isomeric 3-cyano-1-methylpyrazole.The synthesis of the cations and dications from N-aminoazoles was easily performed.The reaction of 1-aminobenzimidazole with dehydroacetic acid in aqueous hydrochloric acid gave not only the expected 1-benzimidazol-1-yl-2,6-dimethylpyridin-4(1H)-one (9), but also 3-acetyl-1-benzimidazol-1-yl-4-hydroxy-6-methylpyridin-2(1H)-one (11).In pyridine, a pyran-2,4-dione intermediate (10), isomeric to (11), was also isolated.The quaternization reactions were easily performed, but high temperatures caused cleavage of the N-N bond.
- Castellanos, Maria Luisa,Llinas, Montserrat,Bruix, Marta,Mendoza, Javier de,Martin, M. Rosario
-
p. 1209 - 1216
(2007/10/02)
-