Synthetic Study of Heteroaromatic Amides as an Agricultural Drug...

合成了多种通式b[1]的杂芳香族酰胺，并对其除草活性进行了研究。通过对水田除草剂的广泛筛选，发现N-[α -（2-噻吩基）-乙基]-4-异丙基苯酰胺[2]对绿藻和蓝藻具有较高的抑制生长活性。以异丙苯和噻吩为原料，开发了一条简洁、经济的四步法合成酰胺[2]的工艺路线。其中一个关键步骤是在甲酸/磷酸的存在下，4-异丙基苯酰胺、噻吩和对甲醛的直接三组分缩合。提出了一种将全氟烷基直接引入各种分子框架的新方法，并成功地应用于含氟杂芳酰胺的合成。

A variety of heteroaromatic amides having a general formula [1] Have been synthesized and their herbicidal activities examined.After extensive screening for paddy field herbicide, N-[alpha-(2-thienyl)-ethyl]-4-isopropylbenzamide [2] Was found to exhibit a high growth-inhibiting activity toward green and blue algae.A concise and economical four-step route to amide [2] has been developed starting from cumene and thiophene. A key step involves the direct three-component condensation of 4-isopropylbenzamide, thiophene and paraaldehyde in the presence of formic acid/phosphoric acid.A novel methodology for introducing perfluoroalkyl group directly into a variety of molecular frames has been developed and successfully employed to the synthesis of fluorine-containing heteroaromatic amides.