Process for preparing 7-¬2-(dialkylamino)ethyl|-4-...

C - Chemistry – Metallurgy – 07 – D

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C07D 235/26 (2006.01) A61K 31/415 (2006.01)

Patent

CA 1255685

ABSTRACT OF THE DISCLOSURE 7-[2-Dialkylamino)ethyl]-4-hydroxy-1,3-benzimidazol- 2-ones having the following structural formula: Image in which: R is hydrogen, and R1 and R2 are, each, C1-C16-alkyl, benzyl, phenethyl or hydroxyphenethyl are prepared by oxidative cyclization of a urea, followed by removal of any protective methyl groups,using a dealkylating agent such as boron tribromide. The compounds are D2-agonists and, thereby, have anti-hypertensive activity. A species produced by this method is 7-[2-(N,N-di-n-propylamino)ethyl]-4- hydroxy-1,3-benzimidazol-2-one.

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