ArticleAngewandte Chemie (International ed. in English)2018
7-Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir.
Article in Angewandte Chemie (International ed. in English), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 18 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
18 citing papers in PubMed, 90 citations in OpenAlex.
- FDA-Approved Drugs Containing Amide Functionality in the Last Five Years (2021-2025): Pharmaceutical Use, Trends and Synthetic Approaches.Medicines (Basel, Switzerland) · 2026Review
- Flow Chemistry Enabled Asymmetric Total Synthesis of (+)-Biotin through Pseudocatalytic Strategy.JACS Au · 2026Article
- Two-Step Synthesis of a Dolutegravir Intermediate DTG-6 in a Microfluidized Bed Cascade System: Route Design and Kinetic Study.Chem & bio engineering · 2025Article
- Synthesis of Dolutegravir Exploiting Continuous Flow Chemistry.The Journal of organic chemistry · 2023Article
- Rapid Enantiomeric Excess Measurements of Enantioisotopomers by Molecular Rotational Resonance Spectroscopy.Organic process research & development · 2023Article
- Recent Developments in the Synthesis of HIV-1 Integrase Strand Transfer Inhibitors Incorporating Pyridine Moiety.International journal of molecular sciences · 2023Review
- A Practical Approach to Bicyclic Carbamoyl Pyridones with Application to the Synthesis of HIV-1 Integrase Strand Transfer Inhibitors.Molecules (Basel, Switzerland) · 2023Article
- The Construction of Polycyclic Pyridones via Ring-Opening Transformations of 3-hydroxy-3,4-dihydropyrido[2,1-Molecules (Basel, Switzerland) · 2023Article
- Understanding flow chemistry for the production of active pharmaceutical ingredients.iScience · 2022Review
- Automated, Multistep Continuous-Flow Synthesis of 2,6-Dideoxy and 3-Amino-2,3,6-trideoxy Monosaccharide Building Blocks.Angewandte Chemie (International ed. in English) · 2021Article
- Preparation of the Key Dolutegravir Intermediate via MgBrMolecules (Basel, Switzerland) · 2021Article
- Telescoped Continuous Flow Synthesis of Optically Active γ-Nitrobutyric Acids as Key Intermediates of Baclofen, Phenibut, and Fluorophenibut.Organic letters · 2020Article
- The evolution of Tamiflu synthesis, 20 years on: Advent of enabling technologies the last piece of the puzzle?Tetrahedron · 2020Review
- Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIV.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Multigram-scale flow synthesis of the chiral key intermediate of (-)-paroxetine enabled by solvent-free heterogeneous organocatalysis.Chemical science · 2019Article
- Continuous flow synthesis of a pharmaceutical intermediate: a computational fluid dynamics approach.Reaction chemistry & engineering · 2019Article
- Enantioselective synthesis ofChemical science · 2019Article
- 7-Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir.Angewandte Chemie (International ed. in English) · 2018Article
Corrections and comments
- Erratum issued
Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Dolutegravir (DTG), an important active pharmaceutical ingredient (API) used in combination therapy for the treatment of HIV, has been synthesized in continuous flow. By adapting the reported GlaxoSmithKline process chemistry batch route for Cabotegravir, DTG was produced in 4.5 h in sequential flow operations from commercially available materials. Key features of the synthesis include rapid manufacturing time for pyridone formation, one-step direct amidation of a functionalized pyridone, and telescoping of multiple steps to avoid isolation of intermediates and enable for greater throughput.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.