Technology platform namely eI2C (expedite ideas to compounds) shown below originates from ArQule’s AMAP technology and is refined to meet changing needs of pharmaceutical R&D. Capability of delivering compounds designed by medicinal chemist for SAR study in accelerated speed helps our clients to advance the program faster and make informed decision earlier and cheaper, without investing infrastructure in high speed medicinal chemistry. Capacity of delivering hundreds of thousands compounds annually ensures Alputon as a global center of excellence in high quality compound design and generation.

The technology platform comprises of instrumentation and informatics infrastructure. A list of automation and analytical instrumentation is illustrated in the following diagram.

Parallel synthesis

Vials placed in 24-well reaction metal block serve as reaction and work-up vessels to replace traditional round bottomed flasks. The standardization allows automation of unit operations such as introduction of reactants and reagents, heating and shaking of reaction mixture, work-up and evaporation. Tecan liquid handlers with customized applications and Genevac with programmed evaporation are major equipments to carry the above mentioned unit operations effectively and efficiently.

Multiple parallel syntheses from tens to hundreds per run can be accomplished within a few days to a week depending on reaction time and steps.

Reaction scales range from tens to hundreds of micromoles, which ensures delivery of final compounds in the amount of up to 50 mg for biological studies.

Hundreds of thousands of compounds can be generated using current capacity while a broad range of reactions such as Suzuki coupling, Mitsunubo reaction, and heterocycle formation have been run successfully on the technology platform.

LC (SFC)-MS purification

Final reaction mixtures in the vials held by reaction blocks are seamlessly plugged into purification process. MS triggered collection provides most efficient purification technology.

Sequential automated purification process requires limited to no attention from scientists after queuing in the purification sequence. It only takes several minutes to purify a compound while superior quality (greater than 95% percent by UV or ELSD) is obtained reliably and consistently.

Mass spectrometers, HPLCs or SFC, Gilson liquid handlers, detectors, and GeneVacs are integrated to perform smooth purification. Based on the systems we have, hundreds of thousands of compounds can be purification annually.

LC-MS characterization and compound reformatting

Compounds after purification are characterized by LC-MS. Compound libraries are reformatted based on pre-set QC standards. The criteria for compound submittal in late stage (such as in the lead optimization) will be more vigorous and greater than 98% of purity can be assured.