METHODS FOR FORMING PROTECTED ORGANOBORONIC ACIDS

• Main Authors: DICK, GRAHAM, R, KLUBNICK, JENNA, A, BURKE, MARTIN, D, GILLIS, ERIC, P, KNAPP, DAVID, M
• Format: Patent
• Language: English; French
• Published: 25.08.2011
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

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. L'invention porte sur des procédés de formation d'acides boroniques protégés qui fournissent d'une manière qui est simple, extensible et économiquement rentable un grand nombre d'éléments structuraux, tels que des éléments structuraux contenant des structures complexes et/ou importantes d'un point de vue pharmaceutique, et/ou qui fournissent des éléments structuraux acides organoboroniques protégés simples ou complexes. Un premier procédé consiste à faire réagir un acide iminodicarboxylique et un sel d'organoboronate. Un second procédé consiste à faire réagir une morpholinedione N-substituée et un acide organoboronique.