New Halogen-Containing Drugs Approved by FDA in 2021: An Overview on Their Syntheses and Pharmaceutical Use

Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

(2022) Zhao Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective electrophilic di- and monofluorinations for the synthesis of 4-difluoromethyl and 4-fluoromethyl quinazolin(thi)ones by a Selectfluor-triggered multi-component reaction

(2022) Ruiqin Zhang et al.   Organic Chemistry Frontiers

Umbralisib, a Dual PI3Kδ/CK1ε Inhibitor in Patients With Relapsed or Refractory Indolent Lymphoma

(2021) Nathan H. Fowler et al.   JOURNAL OF CLINICAL ONCOLOGY

Melphalan Flufenamide (Melflufen): First Approval

(2021) Sohita Dhillon   DRUGS

Ponesimod Compared With Teriflunomide in Patients With Relapsing Multiple Sclerosis in the Active-Comparator Phase 3 OPTIMUM Study

(2021) Ludwig Kappos et al.   JAMA Neurology

Practical Synthesis and Application of Halogen-Doped Pyrrole Building Blocks

(2021) Andrej Emanuel Cotman et al.   ACS Omega

The synthesis review of the approved tyrosine kinase inhibitors for anticancer therapy in 2015–2020

(2021) Xiaoxia Liang et al.   BIOORGANIC CHEMISTRY

Infigratinib: First Approval

(2021) Connie Kang   DRUGS

Piflufolastat F 18: Diagnostic First Approval

(2021) Susan J. Keam   Molecular Diagnosis & Therapy

Fluorine-containing pharmaceuticals approved by the FDA in 2020: Synthesis and biological activity

(2021) Yingjie Yu et al.   CHINESE CHEMICAL LETTERS

Manufacturing Process Development for Belzutifan, Part 5: A Streamlined Fluorination–Dynamic Kinetic Resolution Process

(2021) Tao Wang et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Manufacturing Process Development for Belzutifan, Part 3: Completing a Streamlined Through-Process with a Safe and Scalable Oxidation

(2021) Zhiwei Chen et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Manufacturing Process Development for Belzutifan, Part 4: Nitrogen Flow Criticality for Transfer Hydrogenation Control

(2021) Nastaran Salehi Marzijarani et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Manufacturing Process Development for Belzutifan, Part 2: A Continuous Flow Visible-Light-Induced Benzylic Bromination

(2021) Cecilia Bottecchia et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Manufacturing Process Development for Belzutifan, Part 1: A Concise Synthesis of the Indanone Starting Material

(2021) Feng Peng et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Manufacturing Process Development for Belzutifan, Part 6: Ensuring Scalability for a Deoxyfluorination Reaction

(2021) Michael Pirnot et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Recent Advances in the Application of Selectfluor as a “Fluorine‐free” Functional Reagent in Organic Synthesis

(2020) Ke Yang et al.   Chemistry-An Asian Journal

Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success

(2020) Gene M. Dubowchik et al.   JOURNAL OF MEDICINAL CHEMISTRY

Contribution of Organofluorine Compounds to Pharmaceuticals

(2020) Munenori Inoue et al.   ACS Omega

Editorial Commentary: Tivozanib versus sorafenib in patients with advanced renal cell carcinoma (TIVO-3): a phase 3, multicentre, randomised, controlled, open-label study

(2020) Mary E. Westerman et al.   Annals of Translational Medicine

Tackling Antibiotic Resistance with Compounds of Natural Origin: A Comprehensive Review

(2020) Francisco Javier Álvarez-Martínez et al.   Biomedicines

The prevalence and impact of migraine and severe headache in the United States: Updated age, sex, and socioeconomic‐specific estimates from government health surveys

(2020) Rebecca Burch et al.   HEADACHE

Targeted Drugs for Treatment of Pulmonary Arterial Hypertension: Past, Present, and Future Perspectives

(2020) Wei Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Review of Synthetic Routes and Final Forms of Integrase Inhibitors Dolutegravir, Cabotegravir, and Bictegravir

(2019) David L. Hughes   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Fluorine‐Containing Drugs Approved by the FDA in 2018

(2019) Haibo Mei et al.   CHEMISTRY-A EUROPEAN JOURNAL

Synthetic approaches and pharmaceutical applications of chloro-containing molecules for drug discovery: A critical review

(2019) Wan-Yin Fang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma

(2019) Rui Xu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

(2019) Brian A. Lanman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Umbralisib, a novel PI3Kδ and casein kinase-1ε inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study

(2018) Howard A Burris et al.   LANCET ONCOLOGY

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1

(2018) Joseph Schoepfer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacokinetics and Pharmacodynamics of Cabotegravir, a Long-Acting HIV Integrase Strand Transfer Inhibitor

(2018) Dario Cattaneo et al.   EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS

Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure

(2017) Markus Follmann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors

(2017) Ken A. Brameld et al.   JOURNAL OF MEDICINAL CHEMISTRY

The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1

(2017) Andrew A. Wylie et al.   NATURE

Calcitonin Gene-Related Peptide (CGRP): A New Target for Migraine

(2015) Andrew F. Russo   Annual Review of Pharmacology and Toxicology

An intramolecular C–N cross-coupling of β-enaminones: a simple and efficient way to precursors of some alkaloids ofGalipea officinalis

(2015) Hana Doušová et al.   Beilstein Journal of Organic Chemistry

Does Fluorine Participate in Halogen Bonding?

(2015) Kiamars Eskandari et al.   CHEMISTRY-A EUROPEAN JOURNAL

An Efficient and Highly Diastereoselective Synthesis of GSK1265744, a Potent HIV Integrase Inhibitor

(2015) Huan Wang et al.   ORGANIC LETTERS

Epidemiologie der Multiplen Sklerose in Deutschland

(2014) G. Petersen et al.   NERVENARZT

Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase

(2011) Vito Guagnano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Halogen Atoms in the Modern Medicinal Chemistry: Hints for the Drug Design

(2010) Marcelo Hernandes et al.   CURRENT DRUG TARGETS

2-Imino-thiazolidin-4-one Derivatives as Potent, Orally Active S1P1Receptor Agonists

(2010) Martin H. Bolli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Halogenated Compounds from Marine Algae

(2010) Maria Teresa Cabrita et al.   Marine Drugs

Halogenation Strategies In Natural Product Biosynthesis

(2008) Christopher S. Neumann et al.   CHEMISTRY & BIOLOGY

Use of fluorinated functionality in enzyme inhibitor development: Mechanistic and analytical advantages

(2008) David B. Berkowitz et al.   JOURNAL OF FLUORINE CHEMISTRY

Synthesis and Evaluation of Technetium-99m- and Rhenium-Labeled Inhibitors of the Prostate-Specific Membrane Antigen (PSMA)

(2008) Sangeeta R. Banerjee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fluorine in medicinal chemistry

(2007) Sophie Purser et al.   CHEMICAL SOCIETY REVIEWS