1072833-77-2Relevant articles and documents
A solid-phase approach for the synthesis of α-Aminoboronic acid peptides
Daniels, Blake E.,Stivala, Craig E.
, p. 3343 - 3347 (2018)
A solid-phase synthesis of α-Aminoboronic acid peptides using a 1-glycerol polystyrene resin is described. Standard Fmoc solid-phase peptide chemistry is carried out to construct bortezomib and ixazomib. This approach eliminates the need for liquid-liquid extractions, silica gel column chromatography, and HPLC purifications, as products are isolated in high purity after direct cleavage from the resin.
Virtues of Volatility: A Facile Transesterification Approach to Boronic Acids
Hinkes, Stefan P.A.,Klein, Christian D.P.
supporting information, p. 3048 - 3052 (2019/05/10)
Boronic acids are an increasingly important compound class for many applications, including C-C bond formation reactions, medicinal chemistry, and diagnostics. The deprotection of boronic ester intermediates is frequently a problematic and inefficient step in boronic acid syntheses. We describe an approach that highly facilitates this transformation by leveraging the volatility of methylboronic acid and its diol esters. The method is performed under mild conditions, provides high yields, and eliminates cumbersome and problematic purification steps.
Synthesis and application of peptide borate compounds
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Paragraph 0163; 0208-0209; 0210-0212, (2019/12/25)
The invention belongs to the field of drug synthesis, and specifically relates to a series of novel peptide borate compounds or pharmaceutical salts thereof, and a preparation method and pharmaceutical application thereof. The structure of the peptide borate compounds or the pharmaceutical salts thereof is as shown in a formula I which is described in the specification. The compounds of the invention can be used for preparing proteasome inhibitors, and thus can be further used for treating solid tumors and blood tumors.
