Welcome to Hodoodo Chemicals

Dolutegravir

CAT#: H315142

CAS#: 1051375-16-6

Description: 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.

Synthetic Routes

Dolutegravir - Synthetic Route 1

Synthetic reference

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).

Dolutegravir - Synthetic Route 2

Synthetic reference

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).

Dolutegravir - Synthetic Route 3

Synthetic reference

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).

Dolutegravir - Synthetic Route 4

Synthetic reference

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).

Dolutegravir - Synthetic Route 5

Synthetic reference

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).

Dolutegravir - Synthetic Route 6

Synthetic reference

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).

Dolutegravir - Synthetic Route 7

Synthetic reference

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).

Dolutegravir - Synthetic Route 8

Synthetic reference

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).

Dolutegravir - Synthetic Route 9

Synthetic reference

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).

Dolutegravir - Synthetic Route 10

Synthetic reference

Maras, Nenad; Selic, Lovro; Cusak, Anja. Processes for preparing dolutegravir and cabotegravir and analogues thereof. Assignee Lek Pharmaceuticals D.D., Slovenia. WO 2016113372. (2016).