Asinex Lead Generation

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Discovery Chemistry

ASINEX has developed a trustworthy reputation as a provider of outsourcing since the completion of our first lead optimization project more than 7 years ago. ASINEX provides exclusive library synthesis (may be based on ASINEX IP), multi-step synthesis of challenging compounds, and lead optimization.

Along with standard chemical reactions (i.e. amide coupling, sulfonamide formation reductive animation) which are commonly used for the preparation of large compound libraries, ASINEX chemists are willing to explore a variety of modern synthetic techniques (e.g. boronic acid coupling, phenol and sulphonamide arylation, epoxide opening, C-C coupling reactions, multi-component reactions, nucleophilic aromatic substitution, cycloaddition, cyclisations and heterocycle formations protection-deprotection sequence etc.)

Lead Optimization

ASINEX offers an integrated platform of biology and chemistry skills for hit to lead expansion and lead optimization. We can optimize hits from a multitude of sources and offer an especially fast service for ASINEX's in-house designed compounds. ASINEX can provide design input for template modification and decoration based on known leads and SAR analysis.

Our medicinal chemists with computational biology support teams are able to optimize the following parameters: Intellectual Property, Toxicity, Solubility, Permeability, Metabolism, hERG Electrophysiology etc. ASINEX has a special collection of 2000 highly novel peripheral building blocks which are ideal for improving ADMET features as well as novelty or activity of compounds.

Peripheral Building Blocks for Lead Optimization

Chemistry Expertise

Combinatorial chemistry and parallel synthesis

Hazardous and highly reactive chemicals (HCN, SOCl2, Cl2, COCl2, CO, ClCN, N3-anion)

High pressure reactions (10-100 bar)

Low-temperature reactions

Organometallic reactions (organolithium, Grignard, Heck reactions)

Reductions (catalytic, metal hydrides)

Oxidations (ozone, peroxides, ammoxidation)

Derivatization of natural products

Asymmetric synthesis (transition metal catalysts, biocatalysts, racemate separation)

Custom Synthesis

ASINEX's main area of expertise is hetero-cycle chemistry and challenging multi-step synthesis of small molecule compounds. We can carry out complex synthesis of poly-functional based compounds, use of protection and D-protection techniques, analogues of natural based compounds etc. ASINEX works from milligram to gram scale (up to 200g). Enquiries for scale-up of hit compounds from ASINEX's collections are especially welcome.

Obtaining a quotation from ASINEX for custom synthesis is straight-forward. We would require the chemical structure or catalogue number, the amount of material that you require, the protocol of synthesis or scientific literature available and your preferred deadline for the work.

An English speaking project manager is assigned to every new collaboration, weekly reports shall be promptly provided, regular tele-conferences will be coordinated and face to face meetings as and when required.

Please send your enquires to busdev@asinex.com

HQ Project Management: +7 495 780 3417

ASINEX USA: +1 877 ASINEX1 or +1 336 721 1617
ASINEX Japan: +81-44-400-4428 or +81-80-3401-9097

Once your enquiry has been received by an ASINEX representative, your information will be held in the strictest confidence and you will be contacted within 24 hours. For a detailed quote we usually require 3 working days.