AI Article Synopsis
- A new eco-friendly method has been created to synthesize C2-amino and C2-acyloxy indolin-3-ones using KI as a catalyst and air as the oxidant.
- This process allows for the easy modification of indolin-3-ones at the C2 position, which leads to the creation of 2-substituted variants under mild conditions.
- The technique is applicable to complex pharmaceutical compounds, making it beneficial for medicinal chemistry research and development.
Article Abstract
We have developed an efficient and green strategy for the synthesis of C2-amino indolin-3-ones and C2-acyloxy indolin-3-ones via KI-catalyzed C(sp)-H amination and acyloxylation of indolin-3-ones using air as the oxidant. The reaction provides straightforward access to 2-substituted indolin-3-ones by the direct functionalization of indolin-3-ones at the C2 position under mild conditions. Moreover, the conditions enable direct functionalization of a range of complex pharmaceuticals, providing attractive products for medicinal chemistry programs.
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| http://dx.doi.org/10.1021/acs.orglett.3c03480 | DOI Listing |
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