Dolutegravir, also known as GSK1349572, is a potent inhibitor of HIV integrase with an IC50 value of 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro.1 It inhibits HIV-1 viral replication (EC50 = 0.51 nM) in peripheral blood mononuclear cells (PBMCs). Dolutegravir (DTG) is an antiretroviral medication used, together with other medication, to treat HIV/AIDS. It may also be used, as part of post exposure prophylaxis, to prevent HIV infection following potential exposure.
Aoyama, Yasunori; Hakogi, Toshikazu; Fukui, Yuki; Yamada, Daisuke; Ooyama, Takao; Nishino, Yutaka; Shinomoto, Shoji; Nagai, Masahiko; Miyake, Naoki; Taoda, Yoshiyuki; Yoshida, Hiroshi; Yasukata, Tatsuro. Practical and Scalable Synthetic Method for Preparation of Dolutegravir Sodium: Improvement of a Synthetic Route for Large-Scale Synthesis. Organic Process Research & Development. Volume 23. Issue 4. Pages 558-564. Journal; Online Computer File. (2019).
Wang, Xianheng; Chen, Song; Zhao, Changkuo; Long, Liangye; Wang, Yuhe. Preparation of Dolutegravir Intermediate Diastereomer. Journal of Heterocyclic Chemistry. Volume 56. Issue 7. Pages 2063-2067. Journal; Online Computer File. (2019).
Ziegler, Robert E.; Desai, Bimbisar K.; Jee, Jo-Ann; Gupton, B. Frank; Roper, Thomas D.; Jamison, Timothy F. 7-Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir. Angewandte Chemie, International Edition. Volume 57. Issue 24. Pages 7181-7185. Journal; Online Computer File. (2018).
Rajan, Srinivasan Thirumalai; Eswaraiah, Sajja; Reddy, Ghojala Venkat; Reddy, Sagyam Rajeshwar; Markandeya, Bekkam; Rajesham, Boge. Novel crystalline polymorph of sodium (4R,12aS)-9-{[(2,4-difluorophenyl)methyl]carbamoyl}-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazin-7-olate and process for preparation thereof. Assignee MSN Research & Development Center, India. IN 201641037221. (2018).
Sharma, Pramodkumar; Rao, Bhatraju Srinivasa; Deo, Keshav. A process for the preparation of Dolutegravir or its pharmaceutical acceptable salts thereof. Assignee Wockhardt Limited, India. IN 2015MU01007. (2016).
Weaver, Jimmie Dean. Preparation of fluoroarenes via hydrogen bond directed photocatalytic hydrodefluorination of perfluoroarenes. Assignee The Board of Regents for Oklahoma State University, USA. WO 2018187336. (2018).
Li, Xuguang; Chen, Shuiku; Zhu, Songlin; Zhang, Fangjie; Fang, Shuixia; Liu, Congjun; Zhu, Huifeng; Luo, Qi; Meng, Qingyue; Cui, Hao. Method for preparation of dolutegravir. Kaifeng Pharmaceutical (Group) Co., Ltd.; Henan Furen Pharmaceutical Technology Development Co., Ltd. CN 108299466. (2018).
Vellanki, Sivaram Prasad; Nadella, Madumurthy; Bhalme, Mitali; Ramabhotla, Revathi Srinivas. Process for the preparation of dolutegravir, an integrase inhibitor for HIV-1 infection therapy. Assignee Mylan Laboratories Ltd., India. IN 2015CH00588. (2016).
Sankareswaran, Srimurugan; Mannam, Madhavarao; Chakka, Veerababu; Mandapati, Srirami Reddy; Kumar, Pramod. Identification and Control of Critical Process Impurities: An Improved Process for the Preparation of Dolutegravir Sodium. Organic Process Research & Development. Volume 20. Issue 8. Pages 1461-1468. Journal; Online Computer File. (2016).
Maras, Nenad; Selic, Lovro; Cusak, Anja. Processes for preparing dolutegravir and cabotegravir and analogues thereof. Assignee Lek Pharmaceuticals D.D., Slovenia. WO 2016113372. (2016).
