High Throughput Synthesis of 4-Hydroxy Indole and its Derivatives
© 2024 Mantas Jonušis, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Recently we have been working on 4-OH indole synthesis because it is very interesting heterocycle. For example it is used for the synthesis of indopan - drug for heart problems or anticancer agents. It is also very versatile building block in organic synthesis of other natural and artificial compounds.
Synthesis starts form indenone or substituted indenones. These starting materials are available at Sigma-Aldrich or can be easily synthesized from phenylpropionic acids and polyphosphoric acid byt the further reaction.
Our invention of 4-OH-indole synthesis from indenonoes is previously unpublished approach. We have studied reaction conditions on broad scope of substrates and it seems to work on activated and deactivated indenones.
These findings suggest that it might be the invention of new named reaction. Some more research should be done on mechanism studies.