Sulfated polyborate: mild, efficient and eco-friendly catalyst for the synthesis of 2,3-dihydroquinazolin-4(1H)-ones

Highly efficient and environmental friendly one‐pot synthesis of trisubstituted methanes form aldehydes and heteroaryls with sulfated polyborate catalyst was conveniently performed under solvent‐free grinding condition at room temperature. The catalyst is recyclable up to five consecutive runs and column chromatography‐free isolation of the trisubstituted methanes in excellent yields was achieved.

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Environmentally Benign, Highly Efficient and Expeditious Solvent‐Free Synthesis of Trisubstituted Methanes Catalyzed by Sulfated Polyborate

Jejurkar

Khatri

Chaturbhuj

et al. 2017

ChemistrySelect

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Sulfated Polyborate Catalyzed Improved Synthesis of Enamines and Enaminones Based Intermediates of Imatinib, Nilotinib and Ocinaplon**

2023

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An activation of methyl ketones or active methylenes and N, Ndimethylformamide dimethyl acetal at 110 °C by sulfated polyborate under solvent-free conditions has been developed for enamines and enaminones synthesis. Selected Brønsted acid, optimized reaction conditions, and easy separation method lead to 82-97 % yield, making this process costeffective and eco-friendly. We chose boric acid for scale-up activity in the interest of readers and industries. The optimized reaction condition was applied to demonstrate a 10 gram scale for the intermediate of Imatinib and Nilotinib with an 80 % from 3-acetylpyridine. This method is extendable to produce Ocinaplon intermediate with 80.6 % yield using 4-acetyl pyridine as starting material.

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Rapid and efficient protocol for Willgerodt–Kindler’s thioacetamides catalyzed by sulfated polyborate

2017

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Sulfated polyborate: mild, efficient and eco-friendly catalyst for the synthesis of 2,3-dihydroquinazolin-4(1H)-ones

Cited by 31 publications

References 56 publications

Environmentally Benign, Highly Efficient and Expeditious Solvent‐Free Synthesis of Trisubstituted Methanes Catalyzed by Sulfated Polyborate

Environmentally Benign, Highly Efficient and Expeditious Solvent‐Free Synthesis of Trisubstituted Methanes Catalyzed by Sulfated Polyborate

Sulfated Polyborate Catalyzed Improved Synthesis of Enamines and Enaminones Based Intermediates of Imatinib, Nilotinib and Ocinaplon**

Rapid and efficient protocol for Willgerodt–Kindler’s thioacetamides catalyzed by sulfated polyborate

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