PRODRUG COMPOSITIONS, PRODRUG NANOPARTICLES, AND METHODS OF USE THEREOF
The present invention encompasses prodrug compositions, nanoparticles comprising one or more prodrugs, and methods of use thereof.
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Paragraph 0118
(2016/10/17)
Asymmetric copper-catalyzed synthesis of α-amino boronate esters from N-tert-butanesulfinyl aldimines
A general and efficient new method for the asymmetric synthesis of α-amino boronate esters has been developed. The key step is the Cu(I)-catalyzed addition of bis(pinacolato)diboron to N-tert-butanesulfinyl aldimines, which proceeds in good yields (52-88%) and with very high diastereoselectivities (>96:2) for a variety of aldimine substrates. This method was applied to an efficient synthesis of bortezomib, a potent α-amino boronic acid inhibitor of the proteasome that is in clinical use for the treatment of multiple myeloma and mantle cell lymphoma. Copyright
Beenen, Melissa A.,An, Chihui,Ellman, Jonathan A.
p. 6910 - 6911
(2008/12/22)
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