10.6084/m9.figshare.1416162.v3 Satish Kumar Vujjini Satish Kumar Vujjini Sunitha Vyala Sunitha Vyala Krishna Rao Badarla Krishna Rao Badarla Sreenatha Charyulu Kandala Sreenatha Charyulu Kandala Rakeshwar Bandichhor Rakeshwar Bandichhor Mukkanti Kagga Mukkanti Kagga Praveen Cherukupalli Praveen Cherukupalli Simple and Efficient Process for the Large-Scale Preparation of Agomelatine: An Antidepressant Drug Taylor & Francis Group 2015 sodium diformylamide Key steps Efficient Process nucleophilic displacement Antidepressant Drug scalable process chloroacetyl chloride agomelatine 2015-07-20 18:00:46 Journal contribution https://tandf.figshare.com/articles/journal_contribution/Simple_and_Efficient_Process_for_the_Large_Scale_Preparation_of_Agomelatine_An_Antidepressant_Drug/1416162 <div><p></p><p>A simple and efficient process for the large-scale preparation of agomelatine (<b>1</b>), an antidepressant drug is, described. Agomelatine was prepared in a linear manner starting from readily available, inexpensive 2-naphthol. Key steps in the synthesis are Friedel–Crafts acylation of 2-naphthyl acetate with chloroacetyl chloride, reduction of keto intermediate, and nucleophilic displacement of chloro intermediate with sodium diformylamide. A systemic approach was described to streamline the process into a robust scalable process by controlling the impurities.</p></div>