Ultra-low & high Temperature Technology
Organic fluorides are crucial in pharmaceutical industry.Nearly one fifth of the newly marketed drugs contain fluorine. Fluorinated drugs are usually more efficient on the targeted organs because of better membrane penetration and higher bioavailability, which results in lower daily drug dosage.EOS Med Chem has applied the technology in the syntheses of key intermediates of sofosbuvir and riociguat, as well as spiro,four-, five- and six-membered rings.
Ultra-low temperature reactions are typically highly selective and hence are effective in improving process yield and product purity.The most typical ultra-low& hightemperature reaction is metallation, which is widely used in syntheses of high-valued aromatic boric acid, aldehyde, acid and ester etc. EOS Med Chem has applied ultra-low temperature technology in the synthesis of innovative building blocks,including many four-membered,five-membered and six-membered rings.
Continuous Flow Chemistry
As one of the most promising technologies,continuous flow chemistry is advantageous in improving purity,enhancing yield,simplifying process and ensuring stabilityand safety.
EOS Med Chem has successfully applied the technology in both lab and production,to facilitate our customers’ access to a wider scope of products and services.
EOS Med Chem takes advantage of a large tool kit of chiral catalysts,ligands and auxiliaries etc., to develop asymmetric syntheses of building blocks.
Asymmetric synthesis is effective to cut down production costs, improve reaction efficiency,and reduce wastes and energy consumption per unit of output.
• Asymmetric reduction
• Asymmetric kinetic resolution
• Asymmetric addition
• Asymmetric fluorination
EOS Med Chem Case : In the process development of a key intermediate,an enantioselective fluorination was employed to give high stereo-selectivity,using
a modified cinchona alkaloid catalyst.Further stereo-selective reduction provided a building block with two adjacent chiral centers and greater than 98% ee.
Efficient enzyme catalysts have been used in EOS Med Chem to synthesize high value-added intermediates.The technology enables improved quality,
reduced wastes, lower facility costs and energy consumption.It is prospective to apply enzyme catalysis in a wide range of chemical syntheses of key
intermediates such as chiral alcohols and chiral amines.
• Enzyme catalyzed acylation
• Enzyme catalyzed hydrolysis
• Enzyme catalyzed dynamic kinetic resolution
EOS Med Chem Case : In contrast to regular kinetic resolution, dynamic kinetic resolution can theoretically reach100% yield, which drastically increases the
efficiency and reduces the waste. In one application, we succeeded in obtaining a pyrrolidine building block with two adjacent chiral centers after ones tep
from a racemic mixture in greater than 80% yield.
Photochemical technology is used in the synthesis of innovative building blocks with high strains which are otherwise difficult to prepare.Flow photoreactors
are available at both EOS Med Chem Nanjing andDiai sites.
• Bridged intermediates
• Photochemical oxidation
EOS Med Chem is committed to sustainable chemistr yto protect our environment and human health.We strive to reduce pollution from the source by
minimizing or avoiding the use of hazardous reagents and solvent in the design, development and production of our products.