摘要 |
<P>PROBLEM TO BE SOLVED: To provide a chemical process for preparing [4-(1,3,4-oxadiazol-2-yl) phenyl] boronic acid. <P>SOLUTION: This invention relates to a process for preparing a compound represented by the following formula, wherein, X1 is selected from O, NR1 or S; X2 is selected from CH or N; and R1 is a nitrogen-protecting group. For example, the process includes reacting 2-(4-bromophenyl)-1,3,4-oxadiazole sequentially with (i) methyl-or an optionally substituted aryl-lithium; (ii) n-butyl-, s-butyl-, t-butyl-or n-hexyl-lithium; and (iii) a borate ester. <P>COPYRIGHT: (C)2012,JPO&INPIT |