Organofluorine / Alfa Chemistry
Fluoro-APIs

Fluoro-APIs

Accelerate Innovation with Premium Fluorinated APIs – Available Worldwide

Fluorinated APIs have long played an important role in drug discovery and development, and many fluoro drugs, including fluoxetine, fluticasone, and efavirenz, have been successful drugs with FDA approval. Now more than 25% of marketed drugs include at least one fluorine atom, which indicates the great significance of fluorinated APIs in therapeutics.

At Alfa Chemistry, we design, synthesize, and supply high-quality fluorinated APIs and intermediates using state-of-the-art fluorination techniques and decades of experience in the field of organic fluorine chemistry. If you want to buy fluorinated APIs online, Alfa Chemistry has a large product catalog, custom synthesis services, and global delivery to meet your pharmaceutical needs.

Explore a Comprehensive Catalog of Fluorinated APIs

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Introduction to Fluoro-APIs

Fluorinated APIs are active pharmaceutical ingredients that incorporate fluorine atoms or fluorine-containing groups into their molecular structures. Due to fluorine’s unique electronegativity, small atomic size, and strong C–F bond, these APIs exhibit significantly altered physicochemical and biological properties compared with their non-fluorinated counterparts. Fluorination can enhance lipophilicity, improve protein-binding affinity, modulate pKa values, and fine-tune molecular conformation. These modifications often translate into improved drug potency, metabolic stability, oral bioavailability, and reduced toxicity.

Why Choose Fluoro-APIs?

Improving Pharmacokinetics (ADME)

Fluoride can block metabolic sites and extend half-life.

Improving Metabolic Stability

Strong C-F bonds help resist enzymatic degradation.

Modulating pKa/Electronic Properties

Fluoride's strong electron-withdrawing properties can influence target binding and drug efficacy.

Enhancing Bioavailability

Fluorine substitution can increase membrane permeability and oral absorption.

Optimizing Selectivity

Fluorinated APIs exhibit higher binding affinity and reduced off-target effects.

Building Unique Patent and Chemical Space

Fluorination modifications are often used in differentiated IP strategies.

*These advantages demonstrate the general value of fluorinated APIs in pharmaceutical development, though the actual effectiveness varies depending on the specific compound structure.

Customers Often Look For

Explore our most popular fluorinated APIs, widely used in oncology, infectious diseases, neurology, and metabolic disorders. These representative fluorinated APIs, either approved by regulatory agencies or in clinical development, are recognized for their proven therapeutic value, optimized pharmacokinetics, and proven performance in drug development.

Monofluorinated

Difluorinated

Trifluorinated

CF3-Containing

CF3 + F Substitution

Afatinib

OFC439081182

Trametinib

OFC871700173

Olaparib

OFC763113220

Cabozantinib

OFC849217681

BW-A 78U

OFC101155026

Afatinib

EGFR inhibitor for NSCLC and solid tumors.

Inquiry

Trametinib

MEK inhibitor for metastatic melanoma with BRAFV600E/K mutation.

Inquiry

Olaparib

PARP inhibitor for BRCA-mutated ovarian and breast cancers.

Inquiry

Cabozantinib

Multi-target kinase inhibitor for metastatic thyroid cancer.

Inquiry

BW-A 78U

Experimental PI3K inhibitor for cancer research.

Inquiry

BMS-777607

OFC1025720948

Omipalisib

OFC1086062669

Dolutegravir

OFC1051375166

Entrectinib

OFC1108743607

Ledipasvir

OFC1256388518

BMS-777607

c-Met kinase inhibitor under investigation for solid tumors.

Inquiry

Omipalisib

Dual PI3K/mTOR inhibitor for oncology and fibrosis studies.

Inquiry

Dolutegravir

HIV integrase inhibitor (FDA-approved in 2013).

Inquiry

Entrectinib

TRK/ROS1/ALK inhibitor for NSCLC and solid tumors.

Inquiry

Ledipasvir

NS5A inhibitor for chronic hepatitis C virus (HCV).

Inquiry

Dabrafenib

OFC1195765457

Cobimetinib

OFC934660932

Ivosidenib

OFC1448347496

Mirdametinib

OFC391210109

AG-120 (racemic)

OFC1448346631

Dabrafenib

BRAF V600E inhibitor for melanoma treatment.

Inquiry

Cobimetinib

Selective MEK1/2 inhibitor for solid tumors.

Inquiry

Ivosidenib

IDH1 inhibitor for acute myeloid leukemia (AML).

Inquiry

Mirdametinib

Oral MEK1/2 inhibitor for NF1-associated tumors.

Inquiry

AG-120 (racemic)

Racemate of ivosidenib, IDH1 inhibitor candidate.

Inquiry

Picoxystrobin

OFC117428225

Alpelisib

OFC1217486617

Siponimod

OFC1230487009

JNJ-42153605

OFC1254977871

Upadacitinib

OFC1310726603-1

Picoxystrobin

Strobilurin fungicide targeting mitochondrial respiration.

Inquiry

Alpelisib

PI3Kα inhibitor for breast cancer (FDA-approved 2019).

Inquiry

Siponimod

S1P receptor modulator for multiple sclerosis.

Inquiry

JNJ-42153605

Selective PDE10A inhibitor for neurological disorders.

Inquiry

Upadacitinib

JAK1 inhibitor for rheumatoid arthritis and immune diseases.

Inquiry

Enzalutamide

OFC915087331

Avagacestat

OFC1146699662

Flufenacet

OFC142459583

Enzalutamide

AR antagonist for prostate cancer (FDA-approved 2012).

Inquiry

Avagacestat

γ-secretase inhibitor studied for Alzheimer’s disease.

Inquiry

Flufenacet

Herbicide inhibiting VLCFA synthesis in weeds.

Inquiry

*Click on the links above to explore our popular fluorinated APIs. If you don’t see the compound you need, Alfa Chemistry also offers custom synthesis services to meet your specific project requirements.

Commercial Applications for Fluoro-APIs

The following drug types illustrate the wide commercial application of fluorinated APIs. This includes drug classes across multiple therapeutic areas, which benefit from the attributes fluorine offers to increase potency and selectivity and to enhance pharmacokinetic profiles.

Oncology

Infectious Diseases

Cardiovascular Disorders

Neurology & Psychiatry

Oncology

Fluorinated APIs form the backbone of current cancer therapies, which is why many kinase inhibitors (BRAF inhibitors, MEK inhibitors, EGFR inhibitors, etc. ), PARP inhibitors, and VEGF inhibitors are fluorinated drugs. In oncology, fluorinated APIs are critical for the treatment of lung cancer, breast cancer, ovarian cancer, colorectal cancer, and melanoma, to name a few, and the targeted therapies that have become the standard of care for these conditions with the highest overall survival rates. The worldwide need for cancer therapeutics has made fluorinated drugs some of the most commercially valuable products.

Infectious Diseases

Fluorinated APIs have found application in many antiviral drugs, such as HIV therapies (integrase inhibitors like dolutegravir) and HCV therapies (NS5A inhibitors like ledipasvir), as well as antifungal therapies (such as isavuconazole) for life-threatening invasive infections. Their stability and increased bioavailability make fluorinated APIs a mainstay in the pharmaceutical industry for dealing with drug-resistant microorganisms and effective therapies.

Cardiovascular Disorders

Fluorinated compounds are used in therapeutics for high blood pressure, arrhythmia, and hyperlipidemia. The improvements to PK profiles that fluorine can provide are important for cardiovascular drugs, as they need to be longer-acting to reduce the dosing frequency, which is directly tied to patient compliance and care. The rising global mortality of cardiovascular disease has made fluorinated APIs a necessity for the development of newer and more effective cardiovascular drugs.

Neurology & Psychiatry

Fluorination of compounds has been a critical technique for improving neurological and psychiatric therapeutics, including SSRIs (such as fluoxetine) for depression and anxiety and disease-modifying therapies for multiple sclerosis (such as teriflunomide). These APIs provide great penetration of the blood–brain barrier, greater binding at target receptors, and better tolerability, thus, some of the most commercially attractive APIs for these indications are for the treatment of chronic diseases.

Alfa Chemistry's Core Capabilities for Fluoro-APIs

Off-the-Shelf and Custom Synthesis

We offer a wide range of common fluorinated APIs and intermediates in-stock, while also supporting customized synthesis and method development tailored to customer needs (see Customization Projects below).

Multi-Step Synthesis and Scale-Up Capabilities

We can optimize synthetic routes and scale up processes from mg-scale to pilot/small-scale scale-up.

Chirality Control and Separation

We can synthesize chiral fluorine substitution sites, perform chiral HPLC separations, and perform enantiomeric enrichment.

Diverse Fluorination Reaction Specialties

We offer aryl fluorination, alkyl fluorination, trifluoromethylation, selective fluorination, and nucleic acid/heterocycle fluorination processes.

Analysis and Structure Confirmation

We possess specialized analytical methods for fluorinated compounds (see QC Projects below).

Tailored Fluoro-API Development to Accelerate Your Drug Discovery

Integrating fluorine atoms into complex active pharmaceutical ingredients requires a high level of specialization—both in chemistry and in handling demanding reaction conditions. Alfa Chemistry, with its deep expertise in organofluorine chemistry and state-of-the-art cGMP facilities, can provide end-to-end custom development solutions tailored to your needs.

  • Early-Stage Route Scouting
  • Process Development & Optimization
  • Process Validation, Scale-Up & Tech Transfer
  • Analytical Method Development & Stability Studies
  • Second-Generation Process Development
  • Solubility Enhancement & Formulation Support
  • Core Technologies & Safe Handling Expertise

Learn more

Looking to buy fluorinated APIs online?

At Alfa Chemistry, submit an online inquiry or contact us directly by email or phone for a project evaluation and quote.

Learn about the ordering process

Quality & Compliance

To ensure the reproducibility and traceability of fluorinated APIs, Alfa Chemistry provides rigorous quality management and analytical support (the following and additional tests/documentation may be provided based on project requirements):

Available Documents

  • COA (Batch Report of Analysis)
  • Original chromatograms and spectra (HPLC, NMR, MS)
  • SDS (Safety Data Sheet)
  • GMP/DMF supporting documentation, batch records, and stability data (provided based on project and client contract requirements)

Routine analytical and release testing

  • HPLC/UPLC (purity, quantification of relevant impurities)
  • 1H, 13C, and 19F NMR (structure confirmation, particularly for critical fluorinated sites)
  • HRMS/LC–MS (molecular weight confirmation, impurity identification)
  • Elemental analysis (CHN)
  • Residual solvent determination (compliant with ICH Q3C)
  • Optical purity determination (chiral HPLC or GC, if applicable)
  • Moisture (Karl Fischer) and melting point determination (if applicable)

Learn more about Alfa Chemistry's analytical capabilities

Packaging, Shipping, and Regulatory Considerations

  • We offer a variety of packaging options (light-blocking bottles, nitrogen-filled, cold chain, etc.) based on customer application and shipping requirements.
  • Export/import restricted substances, controlled chemicals, and technology export restrictions require customer compliance confirmation; we will provide the necessary documentation in accordance with regulations.

Customer Case Studies

Case 1: Spot Purchase - BMS-777607 (Fluorinated MET Inhibitor)

A European pharmaceutical company was conducting preclinical studies of an anti-cancer drug candidate and needed to quickly procure 200 g of BMS-777607 (HPLC ≥98%) for metabolic stability and in vivo pharmacokinetic studies.

Solution: Alfa Chemistry provided BMS-777607 in stock (with complete 19F NMR, HRMS, COA, and SDS documentation), and completed quality verification and international cold chain shipping within 5 business days.

Customer Feedback: "Alfa Chemistry's in-stock delivery was fast and reliable, and the analytical data was highly consistent with our internal retesting results, helping us accelerate the advancement of our drug candidate into animal studies."

1025720-94-8

Case 2: Custom Synthesis - Chiral Fluorinated Gefitinib Intermediate

A US biotech company was optimizing the structure of an EGFR inhibitor and required 20 g of a chiral fluorinated gefitinib intermediate (optical purity ≥99% ee).

Solution: Alfa Chemistry delivered a high-purity product within 6 weeks using asymmetric catalytic fluorination combined with chiral HPLC separation. Full chiral NMR and optical purity reports were provided.

Customer Feedback: "This intermediate is difficult to synthesize in-house. Alfa Chemistry's custom synthesis service ensured optical purity, enabling us to quickly complete in vitro cell-based validation."

184475-35-2

Case Study 3: Off-the-Shelf Product + Process Optimization - Fluorinated Imatinib Derivative

An Asian CRO company was commissioned to screen anti-leukemia compounds and required 500 mg of an off-the-shelf fluorinated imatinib heterocyclic derivative. They also wanted to evaluate the feasibility of subsequent kilogram-scale process scale-up.

Solution: Alfa Chemistry provided a small sample of the off-the-shelf product (HPLC ≥98%) and simultaneously conducted process optimization studies, proposing alternative fluorination reagents to improve overall yield.

Customer Feedback: "Off-the-shelf stock meets early screening needs, and process optimization recommendations save significant exploration time and reduce development risk during subsequent scale-up."

152459-95-5

Case Study 4: Custom Synthesis - Fluorinated Atorvastatin Intermediate (kg-Scale)

A multinational pharmaceutical company is advancing process development for a lipid-lowering drug and requires 5 kg of fluorinated atorvastatin intermediate (purity ≥95%, with residual solvents compliant with ICH Q3C).

Solution: Alfa Chemistry's process team achieved stable kg-scale production through a step-by-step fluorination route and provided COA, SDS, batch original spectra, and GMP documentation to ensure regulatory compliance.

Customer Feedback: "Alfa Chemistry demonstrated excellent scale-up synthesis capabilities and a comprehensive documentation system, enabling us to successfully pass internal quality reviews and compliance assessments."

134523-00-5

Frequently Asked Questions (FAQs)

What types of fluorinated APIs can be purchased online?

We offer a wide variety of fluorinated APIs, including mono-, di-, tri-, and CF3-containing compounds. Representative products include afatinib, olaparib, dolutegravir, ledipasvir, dabrafenib, enzalutamide, and regorafenib.

How can I buy fluorinated APIs online at Alfa Chemistry?

A: Submit your compound information and target requirements via the website inquiry form or contact sales directly. We will conduct a feasibility assessment and provide a quote upon receiving the information.

Are Alfa Chemistry's fluorinated APIs suitable for clinical or commercial use?

No. All fluorinated APIs offered by Alfa Chemistry are for research and laboratory use only. They are not intended for human consumption, clinical trials, or commercial production and should be handled according to standard laboratory safety procedures.

Can enantiomeric enrichment of chiral fluorinated APIs be performed?

A: Yes, we have chiral synthesis and separation capabilities, including enantiomeric synthesis, chiral catalysis, and chiral HPLC separations.

What is the minimum order quantity for online orders of fluorinated APIs?

A: The minimum order quantity depends on the chemical properties, synthesis difficulty, and availability. Please provide your target molecule information for evaluation and quotation.

How can I obtain sample spectra and COA?

A: After signing the necessary confidentiality agreement and purchase contract, we will provide COA, HPLC, NMR, and MS data with each batch.