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https://www.ias.ac.in/article/fulltext/jcsc/133/0048 -
Keywords
Tafamidis ;synthesis ;reductive Cyclisation ;zinc-MsOH ;2-aryl benzoxazoles. -
Abstract
A practical zinc-MsOH mediated intra-molecular reductive cyclisation and its application in thesynthesis of tafamidis is presented starting from the readily available 3-hydroxy-4-nitrobenzoic acid as aprecursor. The key reductive cyclization step involves the use of a combination of the readily available zincand MsOH as the catalyst system. This methodology provides an attractive route to 2-aryl benzoxazoles from
ortho-nitro phenols under mild reaction conditions. This methodology is developed on a multi-gram scale andwithout the need for column chromatography.
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Graphical Abstract
A new and alternative zinc-MsOH mediated intra-molecular reductive cyclisation and its application in the synthesis of tafamidis is reported starting from the readily available 3-hydroxy-4-nitrobenzoic acid as precursor. This method provides an attractive route to 2-aryl benzoxazoles from ortho-nitro phenols under mild reaction conditions.
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Author Affiliations
KISHORE KARUMANCHI1 SENTHIL KUMAR NATARAJAN SUNIL GADDE KRISHNA VANCHANAGIRI KRISHNAMURTHY V R MOTURU
- Chemical Research Department, APL Research Centre-II, Aurobindo Pharma Ltd., Survey No. 71 & 72, Indrakaran Village, Kandi Mandal, Sangareddy District 502329, Telangana State, India
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Dates
- Published
- 4 May 2021
- Manuscript received
- 30 October 2020
- Manuscript revised
- 31 January 2021
- Accepted
- 23 March 2021
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Journal of Chemical Sciences
Volume 135, 2023
All articles
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