Biotechnology

①Enzyme screening/improvement technology

When establishing a production route for (1R, 2S)-ethyl 1-amino-2-vinylcyclopropanecarboxylate hemisulfate (VCPA), a pharmaceutical intermediate, we discovered an esterase that enabled the synthesis of the desired monoester starting from a racemic mixture.

Basic concept

A molecular model of the substrate/enzyme complex was constructed and a subsequent screening process was carried out, which identified enzymes with four amino acid substitutions near the active site.

As a result, we introduced mutations at these four points to develop an improved enzyme, which not only has increased optical selectivity in the hydrolysis reaction, but also recognized the differences in the stereochemistry at the position. Consequently, we were able to use the enzyme to prepare solely the desired isomer from the four possible isomers.

(WO2012/029819)

②Various reactions and compounds by biotechnology

We are able to produce compounds such as optically active alcohols, optically active amines, and unnatural amino acids through our hybrid process of biotechnology and organic synthesis.

③Hydroxylated amino acid synthesis technology

Using our company’s hydroxylase library, it is possible to introduce hydroxyl groups at specific locations with high stereoselectivity on amino acid substrates such as cyclic imino acids, basic amino acids, and aliphatic amino acids.

(WO2016/076159)