Industrial (poly)hydroxylates by enzymatic carboligation

Industrial (poly)hydroxylates by enzymatic carboligation


Advantages and Innovations:  FSA variants developed allow: • Exclusive selectivity for the designed single aldol addition, avoiding the formation of byproducts. • Large structural variety of nucleophilic and electrophilic starting materials can be used, especially simple aliphatic ketones and aldehydes. • Capacity to obtain building blocks and products difficult to obtain by conventional chemical methods. • High simplicity and adaptability, with room for on-demand optimization.
Center name:  Тестовый центр
Comments Regarding IPR Status:  European patent application filed in April 2017
Copyright:  Patent(s) applied for but not yet granted
Current Stage of Development:  Several compounds of industrial interest have been prepared using the aldolase, between them Roche ester or of 4-chloro-3-hydroxybutanal
Date of creation:  05/02/2018
Description of the offer:  (Poly)hydroxylate compounds and other related building blocks are high added-value chemicals for the production of market-demanding pharmaceuticals and fine chemicals. Production of (poly)hydroxylate compounds often requires aldol carboligation reactions involving use of hazardous substances and amounts of energy. Development of enzymatic catalysts to carry out stereocontrolled and chemoselective aldol reactions under mild conditions offers a great potential to improve the chemical manufacturing of this type of compounds in compliance with the concept and principles of Green Chemistry. However, current methodologies present restricted substrate selectivity and produce byproduct formation and subsequent reactions that hamper their industrial use. The Spanish and German entities have developed new variants of D-fructose-6-phosphate aldolase from E. coli (FSA) showing high catalytic activity in enantioselective aldol reactions and enabling the production of single (poly)hydroxylate compounds, thereby avoiding byproduct formation. These FSA enzyme variants efficiently catalyze single carboligations of a broad range of substrates (aldehydes and ketones). Particularly interesting for valuable industrial applications are the syntheses, using these enzymes, of the Roche ester or of 4-chloro-3-hydroxybutanal, two key building blocks used for the production of high market value compounds such as statins and other natural products and pharmaceutical compounds. The Spanish and German entities have broad experience in the development of biocatalytic enzymes for industrial sustainable production. They are searching for an industrial company interested in the use of these novel enzyme variants and the methodology associated to manufacture (poly)hydroxylate compounds at industrial scale under a patent licence agreement. Companies interested in this technology should carry out scale-up process to reach the market. The research entities could collaborate with the company in that project.
Market Keywords:  04005 Biochemistry / Biophysics / 08001009 Speciality/performance materials: producers and fabricators / 08001015 Other speciality materials / 08001017 Industrial chemicals
Profile type:  Technology offer
Summary:  A Spanish research institution, a German University and a Spanish company have developed FSA enzyme variants with improved chemo- and enantioselectivity in aldol carboligation reactions (single C-C bond formation) rendering (poly)hydroxylate products of industrial interest, such as Roche ester or of 4-chloro-3-hydroxybutanal, under environmentally friendly conditions. Industrial partners are being sought to collaborate through a patent licence agreement.
Technological Keywords:  02007006 Fine Chemicals, Dyes and Inks / 02007014 Plastics, Polymers / 03004006 Organic Substances / 03004010 Special chemicals, intermediates / 06002003 Enzyme Technology
Type and Role of Partner Sought:  - Partner sought: Industrial producers of fine chemicals and pharmaceuticals to develop and commercialize the technology through a patent licence agreement. - Tasks to be performed by the partner: scale-up and industrial manufacture of (poly)hydroxylated compounds, as intermediate or final products, using the enzymatic catalysts and the methodology developed.
Type of Partnership Required:  License Agreement

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