Biocatalysis, using enzymes for organic synthesis, has emerged as powerful tool for the synthesis of active pharmaceutical ingredients (APIs). The first industrial biocatalytic processes launched in the first half of the last century exploited whole-cell microorganisms where the specific enzyme at work was not known. In the meantime, novel molecular biology methods, such as efficient gene sequencing and synthesis, triggered breakthroughs in directed evolution for the rapid development of process-stable enzymes with broad substrate scope and good selectivities tailored for specific substrates. To date, enzymes are employed to enable shorter, more efficient, and more sustainable alternative routes toward (established) small molecule APIs, and are additionally used to perform standard reactions in API synthesis more efficiently. Herein, large-scale synthetic routes containing biocatalytic key steps toward >130 APIs of approved drugs and drug candidates are compared with the corresponding chemical protocols (if available) regarding the steps, reaction conditions, and scale. The review is structured according to the functional group formed in the reaction.

https://pubs.acs.org/doi/pdf/10.1021/acs.chemrev.1c00574

Shortening Synthetic Routes to Small Molecule Active Pharmaceutical Ingredients Employing Biocatalytic Methods

https://repository.tudelft.nl/islandora/object/uuid%3A9af1f5c4-dee2-4654-a739-474c1b4cf4bd/datastream/OBJ/download

Flavoprotein monooxygenases: Versatile biocatalysts.

Invited for this month's cover is the Working Group Sustainable Chemistry of the European Society of Applied Biocatalysis (ESAB). The image shows the significant contributions of Biocatalysis to science, industry, society, and environment as a technology of first choice for Sustainable Chemistry in the 21st century. The Perspective itself is available at 10.1002/cssc.202102709.

Biocatalysis as Key to Sustainable Industrial Chemistry.

The broad interdisciplinary nature of biocatalysis fosters innovation, as different technical fields are interconnected and synergized. A way to depict that innovation is by conducting a survey on patent activities. This paper analyses the intellectual property activities of the last five years (2014–2019) with a specific focus on biocatalysis applied to asymmetric synthesis. Furthermore, to reflect the inventive and innovative steps, only patents that were granted during that period are considered. Patent searches using several keywords (e.g., enzyme names) have been conducted by using several patent engine servers (e.g., Espacenet, SciFinder, Google Patents), with focus on granted patents during the period 2014–2019. Around 200 granted patents have been identified, covering all enzyme types. The inventive pattern focuses on the protection of novel protein sequences, as well as on new substrates. In some other cases, combined processes, multi-step enzymatic reactions, as well as process conditions are the innovative basis. Both industries and academic groups are active in patenting. As a conclusion of this survey, we can assert that biocatalysis is increasingly recognized as a useful tool for asymmetric synthesis and being considered as an innovative option to build IP and protect synthetic routes.

/pdf/biocatalysis-as-useful-tool-in-asymmetric-synthesis-an-3r60txktuu.pdf

Biocatalysis as Useful Tool in Asymmetric Synthesis: An Assessment of Recently Granted Patents (2014–2019)

Biocatalysis is a highly valued enabling technology for pharmaceutical research and development as it can unlock synthetic routes to complex chiral motifs with unparalleled selectivity and efficiency. This perspective aims to review recent advances in the pharmaceutical implementation of biocatalysis across early and late-stage development with a focus on the implementation of processes for preparative-scale syntheses.

The Evolving Nature of Biocatalysis in Pharmaceutical Research and Development

The present disclosure relates to non-naturally occurring monooxygenase polypeptides useful for preparing prazole compounds, polynucleotides encoding the polypeptides, and methods of using the polypeptides.

Synthesis of prazole compounds

The present disclosure relates to engineered ketoreductase polypeptides and uses thereof for the preparation of α-chloroalcohols from α-chloroketones. Also provided are polynucleotides encoding the engineered ketoreductase polypeptides and host cells capable of expressing the engineered ketoreductase polypeptides.

Ketoreductase-mediated stereoselective route to alpha chloroalcohols

Publisher Summary Chiral heterocycles are of crucial importance to the development and manufacture of new pharmaceuticals and agrochemicals as well as in countless smaller scale applications in synthetic, medicinal, and natural product chemistry. The use of biotransformations to synthesize chiral molecules is building momentum, and biocatalysis is now considered an established approach to such compounds. An increasing number of applications are known, covering a wide array of targets and scales, from the microbial oxidation of drug candidates for metabolite profiling studies to the tons per annum commercial manufacture of agrochemical and pharmaceutical intermediates (APIs). With the advent of directed evolution technologies over the last few years, biocatalysis has emerged as a practical alternative for the large scale synthesis of a range of pharmaceutical intermediates including those for blockbuster drugs, such as Atorvastatin.

Chapter 1: Biocatalytic Approaches to Chiral Heterocycles

The present disclosure relates to engineered ketoreductase polypeptides and uses thereof for the preparation of α chloroalcohols from α chloroketones. Also provided are polynucleotides encoding the engineered ketoreductase polypeptides and host cells capable of expressing the engineered ketoreductase polypeptides.

Polypeptides for a ketoreductase-mediated stereoselective route to alpha chloroalcohols

La presente invention concerne des polypeptides monooxygenases d'origine non naturelle, utiles pour preparer des composes prazoles, sur des polynucleotides codant pour les polypeptides, et sur des procedes d'utilisation des polypeptides.

Synthèse de composés prazoles

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