Synthesis of Some Substituted Pyridines¹

A Practical Synthesis of the PDE4 Inhibitor, SB-207499, from a Cyclohexanone Precursor

“…Hydrolysis of nitrile 6 with Ba(OH) 2 ·8H 2 O gave 7 which had to be purified by reverse phase HPLC in 21% yield. Pure 7 in turn was hydrogenated using Pd/C and ammonium formate as the hydrogen source to give the acids 1 ( 1a : 1b , 96:4). Although this approach required four steps, each step was operationally simple which lowered the cost of the synthesis.…”

Antiallergy agents. 1. Substituted 1,8-naphthyridin-2(1H)-ones as inhibitors of SRS-A release

“…The required nicotinic acids and esters described in Table I, and the substituted amines described in the experimental section were either commercially available or their method of preparation has been described previously.18- 23 The substituted pyridines (3) and congeners described in Table II were prepared by the procedures described by Kermack and Weatherhead24 or Nantka-Namirsky,25 respectively.…”