7‐Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir

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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.

Location: Deutsche Nationalbibliothek Frankfurt am Main

Extent: Online-Ressource

Language: Englisch

Bibliographic citation: 7‐Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir ; volume:57 ; number:24 ; year:2018 ; pages:7181-7185 ; extent:5
Angewandte Chemie / International edition. International edition ; 57, Heft 24 (2018), 7181-7185 (gesamt 5)

Creator: Ziegler, Robert E.
Desai, Bimbisar K.
Jee, Jo‐Ann
Gupton, B. Frank
Roper, Thomas D.
Jamison, Timothy F.

DOI: 10.1002/anie.201802256

URN: urn:nbn:de:101:1-2022090808304816274810

Rights: Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.

Last update: 15.08.2025, 7:25 AM CEST

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Ziegler, Robert E.
Desai, Bimbisar K.
Jee, Jo‐Ann
Gupton, B. Frank
Roper, Thomas D.
Jamison, Timothy F.

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Aufsatzsammlung

Integrase inhibitors

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Synthesis of HIV Integrase Inhibitor MK-1376

HIV drug resistance against strand transfer integrase inhibitors

Update on Adverse Effects of HIV Integrase Inhibitors

Synthesis of an HIV-1 Integrase Allosteric Site Inhibitor

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Multiple choices for HIV therapy with integrase strand transfer inhibitors

Inhibitors of the integrase–transportin-SR2 interaction block HIV nuclear import

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Molecular evolution of HIV-1 integrase during the 20 years prior to the first approval of integrase inhibitors

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7‐Step Flow Synthesis of the HIV Integrase Inhibitor Dolutegravir

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Other Objects (12)

Integrase inhibitors

Synthesis of an Atropisomeric HIV Integrase Inhibitor

Synthesis of an Atropisomeric HIV Integrase Inhibitor

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HIV drug resistance against strand transfer integrase inhibitors

Update on Adverse Effects of HIV Integrase Inhibitors

Synthesis of an HIV-1 Integrase Allosteric Site Inhibitor

Integrase and integration: biochemical activities of HIV-1 integrase

Multiple choices for HIV therapy with integrase strand transfer inhibitors

Inhibitors of the integrase–transportin-SR2 interaction block HIV nuclear import

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

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Integrase inhibitors

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Synthesis of HIV Integrase Inhibitor MK-1376

HIV drug resistance against strand transfer integrase inhibitors

Update on Adverse Effects of HIV Integrase Inhibitors

Synthesis of an HIV-1 Integrase Allosteric Site Inhibitor

Integrase and integration: biochemical activities of HIV-1 integrase

Multiple choices for HIV therapy with integrase strand transfer inhibitors

Inhibitors of the integrase–transportin-SR2 interaction block HIV nuclear import

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

Molecular evolution of HIV-1 integrase during the 20 years prior to the first approval of integrase inhibitors

Integrase inhibitors

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Synthesis of an Atropisomeric HIV Integrase Inhibitor

Synthesis of HIV Integrase Inhibitor MK-1376

HIV drug resistance against strand transfer integrase inhibitors

Update on Adverse Effects of HIV Integrase Inhibitors

Synthesis of an HIV-1 Integrase Allosteric Site Inhibitor

Integrase and integration: biochemical activities of HIV-1 integrase

Multiple choices for HIV therapy with integrase strand transfer inhibitors

Inhibitors of the integrase–transportin-SR2 interaction block HIV nuclear import

Docking studies of flavonoid derivatives as potent HIV-1 integrase inhibitors

Molecular evolution of HIV-1 integrase during the 20 years prior to the first approval of integrase inhibitors

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