€ 5.50 · 4.9 (753) · En stock
Drug leads with a high Fsp3 index are more likely to possess desirable properties for progression in the drug development pipeline. This paper describes the development of an efficient two-step protocol to completely diastereoselectively access a diethanolamine (DEA) boronate ester derivative of monosaccharide d-galactose from the starting material 1,2:5,6-di-O-isopropylidene-α-d-glucofuranose. This intermediate, in turn, is used to access 3-boronic-3deoxy-d-galactose for boron neutron capture therapy (BNCT) applications. The hydroboration/borane trapping protocol was robustly optimized with BH3.THF in 1,4-dioxane, followed by in-situ conversion of the inorganic borane intermediate to the organic boron product by the addition of DEA. This second step occurs instantaneously, with the immediate formation of a white precipitate. This protocol allows expedited and greener access to a new class of BNCT agents with an Fsp3 index = 1 and a desirable toxicity profile. Furthermore, presented is the first detailed NMR analysis of the borylated free monosaccharide target compound during the processes of mutarotation and borarotation.
Molecules, Free Full-Text, chinese wall cpa 20
Molecules, Free Full-Text, kurnik dominó
Download Molecule Royalty-Free Photos, Illustrations, and Vectors
Molecules, Free Full-Text
Molecules, Free Full-Text, Emulsion
What is a Molecule?, Molecules and Matter
Molecule Images - Free Download on Freepik
Molecules, Free Full-Text
Molecules An Open Access Journal from MDPI
Atoms and Molecules Class 9 Notes CBSE Science Chapter 3 [PDF]
Molecules, Free Full-Text, Gum Tragacanth
Chemistry text frame with blue molecule Royalty Free Vector