Described are methods of forming protected boronic acids that provide in a manner that is straightforward, scalable, and cost-effective a wide variety of building blocks, such as building blocks containing complex and/or pharmaceutically important structures, and/or provide simple or complex protected organoboronic acid building blocks. A first method includes reacting an imino-di-carboxylic acid and an organoboronate salt. A second method includes reacting a N-substituted morpholine dione and an organoboronic acid.
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Page/Page column 11; 12
(2011/09/14)
General method for synthesis of 2-heterocyclic N-methyliminodiacetic acid boronates
A wide range of 2-pyridyl and other difficult-to-access heterocyclic N-methyliminodiacetic acid boronates can be readily prepared from the corresponding bromides via a new method involving direct transligation of 2-heterocyclic trialkoxyborate salts with N-methyliminodiacetic acid (MIDA) at elevated temperatures.
Dick, Graham R.,Knapp, David M.,Gillis, Eric P.,Burke, Martin D.
supporting information; experimental part
p. 2314 - 2317
(2010/08/04)
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