A new synthesis of indole 5-carboxylic acids and 6-hydroxy-indole-5- carboxylic acids in the preparation of an o-hydroxylated metabolite of vilazodone
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 carmox
Heinrich, Timo,Boettcher, Henning
p. 2681 - 2684
(2007/10/03)
Synthesis of 3--5-indolecarboxylic Acid, an Antihypertensive Agent with a Novel Mode of Action
The pharmacologically active title compound 1c is prepared in a straightforward six-stage synthesis.The intermediate 4 is obtained by Leimgruber-Batcho indole synthesis.The 3-alkyl side chain is introduced by Friedel-Crafts acylation with 4-chlorobutyryl
Boettcher, Henning,Gericke, Rolf
p. 749 - 752
(2007/10/02)
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