70831-49-1Relevant academic research and scientific papers
MACROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 63; 64, (2020/07/14)
The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.
Phosphite-thioether/selenoether Ligands from Carbohydrates: An Easily Accessible Ligand Library for the Asymmetric Hydrogenation of Functionalized and Unfunctionalized Olefins
Margalef, Jèssica,Borràs, Carlota,Alegre, Sabina,Alberico, Elisabetta,Pàmies, Oscar,Diéguez, Montserrat
, p. 2142 - 2168 (2019/04/13)
A large family of phosphite-thioether/selenoether ligands has been easily prepared from accessible L-(+)-tartaric acid and D-(+)-mannitol and applied in the M-catalyzed (M=Ir, Rh) asymmetric hydrogenation of a broad number of substrates (46 in total). Its highly modular architecture has been crucial to maximize the catalytic performance. Improving most of the reported approaches, this ligand family presents a broad substrate scope. By selecting the ligand parameters high enantioselectivities (ee's up to 99 %) have therefore been achieved in a broad range of both, functionalized and unfunctionalized substrates. Interestingly, both enantiomers of the hydrogenation products can be usually achieved by changing the ligand parameters.
Rapid and scalable synthesis of chiral bromolactones as precursors to α-exo-methylene-γ-butyrolactone-containing sesquiterpene lactones
Lagoutte, Roman,Pastor, Miryam,Berthet, Mathéo,Winssinger, Nicolas
supporting information, p. 6012 - 6021 (2018/09/11)
The sesquiterpene lactones cover a diverse and pharmacologically important diversity space. In particular, the electrophilic α-exo-methylene-γ-butyrolactone moiety that is preponderant in this natural product family has been shown to readily engage in cov
Phosphite-Thiother Ligands Derived from Carbohydrates allow the Enantioswitchable Hydrogenation of Cyclic β-Enamides by using either Rh or Ir Catalysts
Margalef, Jèssica,Pàmies, Oscar,Diéguez, Montserrat
, p. 813 - 822 (2017/02/05)
Phosphite-thioether ligands with a simple modular architecture, derived from inexpensive l-(+)-tartaric acid and d-mannitol, have been for the first time successfully applied (ee values up to 99 %) in the synthesis of 2-aminotetralines and 3-aminochromane
Synthesis of diacylglycerol analogs bearing photoaffinity tags for labelling mammalian diacylglycerol kinase
Eni, Sammy Eni,Rowland, Meng,Best, Michael D.
, p. 25457 - 25461 (2015/03/30)
Signaling lipids such as diacylglycerol (DAG), phosphatidic acid, and the phosphatidylinositol polyphosphates are site-specific ligands for protein binding partners. Herein, we report the apotheoses of our initial approach to the development of diverse probes which are vital for understanding lipid-protein interactions. When incorporated into liposomes, these probes reduce mammalian diacylglycerol kinase's (DGK) enzymatic activity in a concentration, time, and light dependent manner. This journal is
Versicolactones A and B: Total synthesis and structure revision
Wang, Liping,Zhu, Weiming
, p. 6729 - 6731 (2013/11/19)
To further determine absolute configurations of versicolactones A and B, total synthesis of versicolactones A and B and their six stereoisomers were reported in this Letter. The 1H and 13C NMR spectra of the synthetic erythro-stereoisomers matched perfectly with those of the natural products. Combined with the comparison of the specific rotations, the absolute configuration of versicolactones A and B were revised as (4Z,6R,7S)- and (4E,6R,7S)- from the corresponding (4Z,6R,7R)- and (4E,6R,7R)-6,7-dihydroxyocta- 2,4-dien-4-lactone, respectively.
AMPHIPHILIC COMPOUNDS AND SELF-ASSEMBLING COMPOSITIONS MADE THEREFROM
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, (2012/03/12)
The present disclosure relates to amphiphilic compounds, self assembling compositions formed from the amphiphilic compounds and methods of making such compositions.
Intramolecular Huisgen [3+2] cycloaddition in water: Synthesis of fused pyrrolidine-triazoles
Kumar, Indresh,Mir, Nisar A.,Rode, Chandrashaker V.,Wakhloo, Basant P.
experimental part, p. 225 - 229 (2012/06/18)
The intramolecular alkyne-azide Huisgen [3+2] cycloaddition reaction as a 'click-chemistry' reaction without a metal catalyst has been studied under aerobic conditions. The synthesis of various pyrrolidine-triazole hybrid compounds has also been achieved
Synthesis of hybrid 1,2,3-triazolo-δ-lactams/lactones using Huisgen [3+2] cycloaddition 'click-chemistry' in water
Kumar, Indresh,Rana, Sravendra,Cho, Jae Whan,Rode, Chandrashekhar V.
scheme or table, p. 352 - 355 (2010/06/16)
The synthesis of a new class of hybrid 1,2,3-triazozlo-δ-lactams/lactones has been achieved using the Huisgen [3+2] dipolar cycloaddition 'click-chemistry' reaction of various organic azides with an activated alkyne in water, followed by cyclization.
Total synthesis of (+)-varitriol
Palik, Miroslav,Karlubikova, OL'Ga,Lasikova, Angelika,Kozisek, Jozef,Gracza, Tibor
scheme or table, p. 709 - 715 (2009/07/19)
The total synthesis of natural (+)-varitriol (1) was accomplished by starting from dimethyl L-tartrate. The key features were a substrate selective and diastereoselective PdII-catalysed bicyclisation of unsaturated protected triol 9 followed by regioselective ring-opening of bicyclic skeleton 10. The absolute configuration of the target was confirmed by single-crystal X-ray analysis for the first time.
