A convenient and practical prepapation of acetylphenyl boronic acids

A practical and scalable synthesis route of acetylphenylboronic acids is described. Bromoacetophenones (compounds 3a, 3b) were ketalized with ethylene glycol and triethyl orthoformate to give bromo ketals(compounds 4a-4c) in 60-80% yields. Compounds 4a-4b were treated with a Grignard reagent and then exchanged with borate to give p- and m-acetylphenyl boronic acids(compounds 5a and 5b) in 80% and 56% yields, respectively. The o-form(compound 5c) was obtained in 61% yield via the BuLi method.Chemistry, MultidisciplinarySCI(E)EI中国科学引文数据库(CSCD)0ARTICLE6734-7372