Paladugu, Srinu ; Mainkar, Prathama S. ; Chandrasekhar, Srivari (2018) Synthesis of Asthma Drug Zafirlukast (Accolate) Using Intramolecular Oxidative Coupling via sp3 C–H Bond Activation ACS Omega, 3 (4). pp. 4289-4294. ISSN 2470-1343
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Official URL: http://doi.org/10.1021/acsomega.8b00476
Related URL: http://dx.doi.org/10.1021/acsomega.8b00476
Abstract
The FDA-approved drug for the treatment of asthma, zafirlukast, is synthesized engaging multiple catalytic reactions including a new method for the construction of 3-aroylindoles via oxidative cyclization. The highlights include transition-metal and peroxide free C–H bond activation using the stoichiometric amount of sodium persulfate as an oxidizing agent in the construction of 3-aroylindole, avoiding transition metal, with over 28% overall yield. The complete process has a turnaround time of 28 h to get the target molecule starting from substituted aniline, with practically no protecting groups.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to American Chemical Society |
| ID Code: | 131294 |
| Deposited On: | 06 Dec 2022 09:15 |
| Last Modified: | 06 Dec 2022 09:15 |
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