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

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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.