Fluorine-containing drugs approved by the FDA in 2021

J He, Z Li, G Dhawan, W Zhang, AE Sorochinsky… - Chinese Chemical …, 2023 - Elsevier
Nine new fluorine-containing drugs have been approved by the US Food and Drug
Administration (FDA) in 2021, which are presented in this review article. These small …

New halogen-containing drugs approved by FDA in 2021: An overview on their syntheses and pharmaceutical use

D Benedetto Tiz, L Bagnoli, O Rosati, F Marini… - Molecules, 2022 - mdpi.com
This review describes the recent Food and Drug Administration (FDA)-approved drugs (in
the year 2021) containing at least one halogen atom (covalently bound). The structures …

Fluorine-a small magic bullet atom in the drug development: perspective to FDA approved and COVID-19 recommended drugs

G Chandra, DV Singh, GK Mahato, S Patel - Chemical Papers, 2023 - Springer
During the last twenty years, organic fluorination chemistry established itself as an important
tool to get a biologically active compound. This belief can be supported by the fact that every …

Resonance‐assisted hydrogen bonding as a driving force in synthesis and a synthon in the design of materials

KT Mahmudov, AJL Pombeiro - Chemistry–A European …, 2016 - Wiley Online Library
Resonance‐assisted hydrogen bonding (RAHB), a concept introduced by Gilli and co‐
workers in 1989, concerns a kind of intramolecular H‐bonding strengthened by a …

7‐step flow synthesis of the HIV integrase inhibitor dolutegravir

RE Ziegler, BK Desai, JA Jee, BF Gupton… - Angewandte …, 2018 - Wiley Online Library
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 …

Review of synthetic routes and final forms of integrase inhibitors dolutegravir, cabotegravir, and bictegravir

DL Hughes - Organic Process Research & Development, 2019 - ACS Publications
Bictegravir and dolutegravir are two recently approved integrase inhibitors for the treatment
of HIV. A third inhibitor, cabotegravir, is in Phase 3 development. As a continuation of a …

Control over selectivity for demethylation in dolutegravir synthesis in microreactors: Kinetics and mechanisms

X Xue, C Xie, G Qian, M Qiu, R Jiang, M Pasha… - Chemical Engineering …, 2024 - Elsevier
Abstract Demethylation of DTG-7 (ie, an intermediate of an anti-HIV medication dolutegravir
(DTG)) is the final step in the DTG synthesis, but its reaction network and kinetic …

Synthetic approaches and application of clinically approved small-molecule anti-HIV drugs: an update

L Sun, P Nie, L Luan, P Herdewijn, YT Wang - European Journal of …, 2023 - Elsevier
Application of chemotherapeutic agents to inhibit the HIV replication process has brought
about a significant metamorphosis in the landscape of AIDS. Substantial declines in …

Rapid quantification of isomeric and dehalogenated impurities in pharmaceutical raw materials using MRR spectroscopy

JL Neill, AV Mikhonin, T Chen, RE Sonstrom… - … of Pharmaceutical and …, 2020 - Elsevier
We demonstrate the application of molecular rotational resonance (MRR) spectroscopy to
quantify regioisomeric, dehalogenated, and enantiomeric impurities in two raw materials …

Enantioselective synthesis of gem-disubstituted N-Boc diazaheterocycles via decarboxylative asymmetric allylic alkylation

AW Sun, SN Hess, BM Stoltz - Chemical Science, 2019 - pubs.rsc.org
An enantioselective synthesis of diverse N4-Boc-protected α, α-disubstituted piperazin-2-
ones using the palladium-catalyzed decarboxylative allylic alkylation reaction has been …