The present invention relates to a process for the preparation of crisaborole of formula (I): ##STR00001## by preparing intermediates of formulas (II) and (III): ##STR00002##

Provided herein are novel synthetic compounds having the structure of formula (1), ##STR00001## wherein X is a substituted or unsubstituted aromatic or heteroaromatic mono- or polycyclic ring system; and Y is substituted or unsubstituted C.sup.5-C.sup.10 alkyl or alkenyl group, or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions. The compounds and pharmaceutical compositions are useful for inhibiting growth of a bacterium.

A vinylbenzylated phenol compound represented by General Formula (1) below is provided. ##STR00001##
(In General Formula (1), Ar.sup.0 is a bifunctional phenol compound residue having one or more monocyclic or polycyclic aromatic nuclei, R.sup.1 to R.sup.5 may be the same or different and are each hydrogen or a methyl group, and p is an integer of 1 to 4.)

In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions.

In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions.