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Methods and systems for forming boronic acids and intermediates thereof

  • US 9,145,428 B2
  • Filed: 09/14/2012
  • Issued: 09/29/2015
  • Est. Priority Date: 09/14/2011
  • Status: Active Grant
First Claim
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1. A method of forming a 4-choloro-2-fluoro-3-methoxyphynylboronic acid, comprising:

  • minimizing decomposition of a 6-chloro-2-fluoro-3-lithioanisole by applying a continuous process of forming a 4-choloro-2-fluoro-3-methoxyphynylboronate, wherein the process comprises;

    (i) continuously adding a 2-chloro-6-fluoroanisole and at least one alkyllithium to a first reactor to form the 6-chloro-2-fluoro-3-lithioanisole, while continuously transferring the formed 6-chloro-2-fluoro-3-lithioanisole from the first reactor into a second reactor; and

    (ii) continuously adding a borate to the second reactor, wherein the borate reacts with the 6-chloro-2-fluoro-3-lithioanisole to form the 4-choloro-2-fluoro-3-methoxyphynylboronate, while continuously transferring the formed 4-choloro-2-fluoro-3-methoxyphynylboronate from the second reactor into a receiving container to maintain a reaction mixture volume within the second reactor,wherein the first and the second reactors are maintained at a temperature of less than about −

    50°

    C.; and

    converting the 4-choloro-2-fluoro-3-methoxyphynylboronate to the 4-choloro-2-fluoro-3-methoxyphynylboronic acid.

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