A new synthesis of indole 5-carboxylic acids and 6-hydroxy-Indole-5-carboxylic acid (cas 1670-81-1)s in the preparation of an o-hydroxylated metabolite of vilazodone

Add time:09/28/2019    Source:sciencedirect.com

A major metabolite of the potential antidepressant vilazodone formed in rat, dog, monkey and human liver microsomes is the 5-cyano-6-hydroxy-1H-indole derivative. For the construction of the salicyl-like substituted indole we adapted a synthesis of carmoxirole using Japp–Klingemann type Fischer-indole synthesis protocols. Functional group interconversion of carboxylic acid via carboxamide into cyanide was performed with methanesulfonic acid chloride.

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