6-取代苯并噻唑-2-氨基硫代磷酸二烷基酯的合成

Synthesis of N-(Benzothiazol-2-yl-aminodialkyl)-thiophosphate

用 6-位取代的 2 -氨基苯并噻唑与三氯硫磷反应 ,合成了 3个苯并噻唑 -2 -氨基硫代磷酰二氯 ,并由此合成了 9个苯并噻唑 -2 -氨基硫代磷酸二烷基酯 .讨论了苯并噻唑环上取代基对反应的影响和产物中硫代磷酸酯的烷基的空间效应对反应的影响 .所合成的部分化合物对人喉鳞状细胞癌 ( Hep-2 )具有一定的抑制能力 .

In order to search for highly active anticancer agent,a new type of aminodialkylthiophosphates containing a benzothiazole group was synthesized by two-step reactions. All products were characterized by 1H NMR, 31 P-NMR and elemental analyses. The results of bioassay show that compounds 2a,2b,2c and 2d have some inhibitory effect against humanlaryngocarcinoma(squamous).