Benzofurans and a novel method of preparation

C - Chemistry – Metallurgy – 07 – D

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260/361.1

C07D 307/79 (2006.01)

Patent

CA 1291487

-0- NOVEL BENZOFURANS AND A NOVEL METHOD OF PREPARATION ABSTRACT There are disclosed novel benzofurans having the following structural formula: Image wherein R is alkenyl of 1 to 6 carbon atoms or aryl of from 6 to 10 carbon atoms; R1 is H, alkali metal, or alkyl of 1 to 4 carbon atoms; and R2 is alkyl or alkoxy of from 1 to 5 carbon atoms, hydrogen, amino or dialkylamino, nitro, sulfonyl, alkyl or aryl thioether or halo. Also disclosed is a novel process of making the benzofurans, comprising the step of cyclizing an o-(2-carboxyvinyl)phenyl unsaturated alkyl ether in the presence of a base selected from the group consisting of KOH, NaOH, LiOH, dimsyl sodium, lithium diisopropylamide, potassium text-butoxide, and mixtures thereof, at room temperature. The benzofurans are useful starting materials in forming acetamidine derivatives having pharmacological utility.

544664

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