Synthetic process of 5-Hydroxymethylthiazole

As an important medicine and pesticide intermediate,5-Hydroxymethylthiazole can be furthermore used in the synthesis of the second generation of anti-AIDS drugs Ritonavir.After studying,we obtained an improved process which synthesized 5-hydroxymethylthiazole by taking 2-chloro-5-chloromethylthiazole as raw material and through hydrolysis and reductive de-chlorination.The optimum process conditions were as follows: first,at 75 ℃,2-chloro-5-chloro-methylthiazole(0.05 mol) was hydrolyzed with activated strong alkali anion exchange resin(22.4 g) and 50 mL aqueous solution,the react time was 3.5 hours,and the resins could be repeatedly used twice;second,the obtained 2-Chloro-5-Hydroxymethylthiazole was dechlorinated with hydrazine hydrate and 10% Pd/C of 2.0 g as catalyst,mole ratio of reactants of 2-Chloro-5-Hydroxymethylthiazole and hydrazine hydrate was 1︰3,the Pd/C could be re-used 4 times,the reaction time was 1 hour.The results show that the total yield rate of 5-Hydroxymethylthiazole was 70.44%,w(5-Hydroxymethylthiazole)≥99%(GC,peak area normalization method).The structure of 5-Hydroxymethylthiazole was confirmed by element analysis,IR,LC-MS,1H-NMR and 13C-NMR.