This invention discloses a multifunctionalized
pyridine compound, its preparation method, and its applications, belonging to the fields of pharmaceutical intermediates and
organic synthesis. The invention uses α-allyl-p-toluenesulfonylmethylene isonitrile and substance A as raw materials, and a free
radical cyclization reaction is carried out under the action of a catalyst to obtain a highly functionalized
pyridine compound, as shown in formula (Ⅰ). Substance A is
phenylboronic acid, cyclohexylboronic acid, [1,1'-
biphenyl]-4-
boronic acid, p-methylphenylboronic acid, m-methylphenylboronic acid, o-methylphenylboronic acid, p-cyanophenylboronic acid,
thiophene-3-
boronic acid, or cyclopropylboronic acid. The method of this invention not only has very broad substrate tolerance, inexpensive and readily available raw materials, and a simple reaction process suitable for large-scale synthesis, but also provides a new method for pharmaceutical
chemical synthesis. Furthermore, due to the high functionalization and special structure of the
pyridine compound, it exhibits better
efficacy in treating chronic
stable angina pectoris, central respiratory depression and circulatory failure, and in the treatment of various organoiodinated
phosphate poisonings.