2-氨基-5-甲基噻唑的合成及应用研究

Study on the Synthesis and Using of 2-Amino-5-Methylthiazole

以 1,2 ,3-三氯丙烷为原料 ,与氢氧化钠反应生成 2 ,3-二氯 - 1-丙烯 (2 ) ,接着与硫氰酸钾反应并异构化生成 2 -氯 - 2 -丙烯基异硫氰酸酯 (3) ,再与氨水反应得 N- (2 -氯 - 2 -丙烯基 )硫脲 (4) ,然后再在 80 %的硫酸作用下环合得 2 -氨基 - 5 -甲基噻唑 (1) ,总收率由文献报道的 2 4 .3%提高到 4 1.3%。利用 (1)和吡罗昔康的中间体 (5 )缩合制得美洛昔康 (6 )

amino 5 methylthiazole (1) was prepared using 1,2,3 trichloropropane as starting material, which reacted with sodium hydroxide to get 2,3 dichloro 1 propene ,which reacted with potassium thiocyanide, then via isomerization and reacted with ammonia hydroxide, and at last through cyclization. The overall yield was increased from 24.6% to 41.3%. and Meloxicam(6) was also synthetised by the condensation with 2 amino 5 methylthiazole(1) and the intermediate (5) of piroxicam.