Synthesis of Asthma Drug Zafirlukast (Accolate) Using Intramolecular Oxidative Coupling via sp3 C–H Bond Activation | Zendy

Srinu Paladugu | Zendy; Prathama S. Mainkar | Zendy; S. Chandrasekhar | Zendy

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Synthesis of Asthma Drug Zafirlukast (Accolate) Using Intramolecular Oxidative Coupling via sp³ C–H Bond Activation

Author(s) -

Srinu Paladugu,

Prathama S. Mainkar,

S. Chandrasekhar

Publication year - 2018

Publication title -

acs omega

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.779

H-Index - 40

ISSN - 2470-1343

DOI - 10.1021/acsomega.8b00476

Subject(s) - zafirlukast , oxidizing agent , aniline , persulfate , intramolecular force , chemistry , yield (engineering) , catalysis , combinatorial chemistry , oxidative phosphorylation , stoichiometry , medicinal chemistry , organic chemistry , materials science , antagonist , biochemistry , metallurgy , receptor

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.

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