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Our Key Technologies

Asymmetric Synthesis

PharmaBlock 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


PharmaBlock 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.

Enzyme Catalysis

Efficient enzyme catalysts have been used in PharmaBlock 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


PharmaBlock Case: In contrast to regular kinetic resolution, dynamic kinetic resolution can theoretically reach 100% 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 one step from a racemic mixture in greater than 80% yield.


Photochemical Technology

Photochemical technology is used in the synthesis of innovative building blocks with high strains which are otherwise difficult to prepare.

  • Bridged intermediates
  • Cubanes
  • Photochemical oxidation

Ultra-low Temperature Technology

Ultra-low temperature reactions are typically highly selective and hence are effective in improving process yield and product purity. The most typical ultra-low temperature reaction is metallation, which is widely used in syntheses of high-valued aromatic boric acid, aldehyde, acid and ester etc.

 

PharmaBlock has applied ultra-low temperature technology in the synthesis of innovative building blocks, including many four-membered, five-membered and six-membered rings.

Fluorination

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. PharmaBlock has applied the technology in the syntheses of key intermediates of sofosbuvir and riociguat, as well as spiro, four-, five- 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 stability and safety. 

PharmaBlock has successfully applied the technology in both lab and production, to facilitate our customers’ access to a wider scope of products and services.

Green Chemistry

PharmaBlock is committed to sustainable chemistry to 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.