- An Efficient Benzoxaborole One-Pot Synthesis by SiliaCat DPP-Pd Heterogeneous Catalysis using Diboronic Acid
-
Organoboron compounds are valuable molecules of increasing interest in organic synthesis, catalysis, biology and medicine. Among them, benzoxaboroles emerged as promising building blocks for numerous research programs. In this letter, we communicate the development of new conditions for the one-pot benzoxaborole synthesis by SiliaCat DPP?Pd catalysis using diboronic acid as the boron source. This low cost and sustainable strategy permitted the preparation of a useful range of benzoxaborole building blocks. Finally, the transformation was extended to a continuous flow process using our Vapourtec system. (Figure presented.).
- Kunihiro, Kana,Dumais, Laurence,Lafitte, Guillaume,Varvier, Emeric,Tomas, Lo?c,Harris, Craig S.
-
-
Read Online
- TNIK MODULATORS, CONJUGATES, AND USES THEREOF
-
TNIK inhibitors, conjugates thereof, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. The disclosed compounds are useful, among other things, in treating of cancer by modulating TNIK activity.
- -
-
Paragraph 0373; 0375
(2019/05/10)
-
- A convenient one-pot synthesis of boroxoles from diboronic acid
-
The preparation of the boroxole motif traditionally relies on a 3-step process and the use of n-butyl lithium that can limit substrate scope. Herein during our exploration toward novel RORγ inhibitors, we identified a convenient one-pot preparation of the motif in good yields with good substrate scope.
- Lafitte, Guillaume,Kunihiro, Kana,Bonneaud, Céline,Dréan, Bénédicte,Gaigne, Frédéric,Parnet, Véronique,Pierre, Romain,Raffin, Catherine,Vatinel, Rodolphe,Fournier, Jean-Fran?ois,Musicki, Branislav,Ouvry, Gilles,Bouix-Peter, Claire,Tomas, Loic,Harris, Craig S.
-
supporting information
p. 3757 - 3759
(2017/09/12)
-
- Ring structure and aromatic substituent effects on the p K a of the benzoxaborole pharmacophore
-
In this work, we present an investigation into the physical properties of a unique class of aromatic boronic acids, the benzoxaboroles. Using spectrophotometric methods, the ionization constants of a family of substituted benzoxaboroles are determined. He
- Tomsho, John W.,Pal, Arnab,Hall, Dennis G.,Benkovic, Stephen J.
-
supporting information; experimental part
p. 48 - 52
(2012/04/10)
-
- BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENT
-
This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. The compounds are of the formula, wherein Y' is a halogen, Y is halosubstituted alkyl, or a salt thereof.
- -
-
Page/Page column 78
(2011/10/10)
-
