Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

Abstract

Process for the Preparation of Dolutegravir Intermediate: (R)-3-Amino Butanol

Author(s): Sureshbabu Jayachandra, Madhuresh K Sethi, Vipinkumar Kaushik, Vijayakrishna Ravi, Sanjay Mahajan, Bhairaiah Mara, Gurleen Kaur, Purbita Chakraborty

Dolutegravir, a second-generation HIV Integrase Strand Transfer Inhibitor (INSTI), is the most current antiretroviral ratified for treatment of HIV-1 infection. This approval is based on the superiority of Dolutegravir in clinical trials over the well-known antiretroviral marketed drugs like Efavirenz, Raltegravir, and Darunavir. Largely, Dolutegravir has established excellent tolerability, limited drug interactions, insignificant drug resistance and once-daily dosing for treatment-naive patients. (R)-3-amino butanol is a key unit for the synthesis of Dolutegravir and rarer methods of synthesis are mentioned in the literature.


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