#91 Development of novel synthetic methodologies from aryl ketones and its application in API’s synthesis

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Ghodse, S. . #91 Development of Novel Synthetic Methodologies from Aryl Ketones and Its Application in API’s Synthesis. J Pharm Chem 2022, 8.

Abstract

There has been a very high demand for API intermediates to synthesize drugs in recent years. Carbonyl functionality is an essential precursor for drugs and their intermediates synthesis in the pharmaceutical industry. Most widely used carbonyl groups to prepare carboxylic acid, ester, aldehyde, ketones, amine, and amide APIs. We choose carbonyl ketones as a critical starting material for the synthesis of API’s Intermediate because of its stability, cheapness, ease of handling, and wide applications in pharmaceutical industries such as an excipient, reaction solvents, synthetic fiber, and medicines. We have developed simple, efficient synthetic routes for the critical heterocyclic nucleus such as 2-aminothiazole, 2-phenyl pyridine, and α-N-heteroaryl ketone. Representative drugs which contain 2-aminothiazole are meloxicam (NSAID), 2-phenyl pyridine is etoricoxib (COX Inhibitor), and α-Nheteroaryl ketone is econazole (azole antifungal). In 2020, these drugs will be commonly prescribed medication in the United States, with more than 34 million prescriptions. Results of the following invented methodologies will be presented, with their pharmaceutical applications in drug synthesis of

  1. 2-aminothiazole from aryl ketone
  2. 2-aryl pyridine from aryl ketones
  3. α-N-heteroaryl ketone from aryl ketone

References

Ghodse SM, Telvekar VN. (2015) Synthesis of 2-aminothiazole derivatives from easily available thiourea and alkyl/aryl ketones using aqueous NaICl2. Tetrahedron Lett 56(2):472-474. DOI: https://doi.org/10.1016/j.tetlet.2014.11.140

Ghodse SM, Telvekar VN. (2017) Synthesis of 2-phenyl pyridine derivatives from aryl ketones and 1, 3-diaminopropane using palladium acetate as a catalyst. Tetrahedron Lett 58(6):524-526. DOI: https://doi.org/10.1016/j.tetlet.2016.12.075

Ghodse SM, Hatvate NT, Telvekar VN. (2021) One pot synthesis of α‐N‐heteroaryl ketone derivatives from aryl ketones using aqueous NaICl2. J Heterocycl Chem 1. DOI: https://doi.org/10.1002/jhet.4412

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