Synthesis of 5-(substituted alkyl)picolinic acids. The dopamine .BETA.-hydroxylase inhibitors. II.

Abstract
The improved synthesis of 5-(4-chlorobutyl)picolinic acid (II), the potent dopamine .beta.-hydroxylase inhibitor, was reported. The key intermediate, 2-cyclopropyl-5-cyclopropylcarbonylpyridine was converted to 5-(4-chlorobutyl)-2-cyclopropylpyridine, which was directly oxidized with nitric acid to give II. Similarly, fusaric acid (I) was synthesized from 2-cyclopropyl-5-(cyclopropylhydroxy)methylpyridine. I and II were tested for their hypotensive activity.

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