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Drug Design, Synthesis, and Development
Published in Nathan Keighley, Miraculous Medicines and the Chemistry of Drug Design, 2020
In many cases, the stereochemistry of the drug molecule is of critical importance. Consequently, the synthetic strategy needs to account for stereochemistry in regards to the starting materials being used and the stereoselectivity of the chemical reactions utilised in the synthetic strategy. Often an asymmetric synthesis is required, which will involve specific reagents and chemical processes.
Ene-Reductases in Pharmaceutical Chemistry
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Many drug candidate molecules contain at least one chiral center and consequently, the development of effective asymmetric synthesis methods is essential for the pharmaceutical industry. Besides the well-established metal- and organocatalytic approaches, biocatalytic strategies are being more and more considered to install chirality. Today, the production of several blockbuster drugs such as sitagliptin (Savile et al., 2010) and Montelukast (Liang et al., 2010) has been considerably improved by switching from a purely chemical to a chemoenzymatic set-up. In the early days of industrial biocatalysis, the use of hydrolases dominated the budding discipline due to the enzymes’ high stability and ease of handling; however, significant progress in the field of enzyme engineering facilitated access to robust and easy‐to‐handle oxidoreductases and transaminases which are now established tools in the synthesis of enantiopure alcohols and amines (Bornscheuer et al., 2012). This trend is also reflected by the increasing number of patents filed for biocatalytic applications in industry (Buller et al., 2018).
Radioactivity and Radiotracers
Published in Graham Lappin, Simon Temple, Radiotracers in Drug Development, 2006
More recently, there has been a demand for optically-pure 14C-compounds, as opposed to racemic mixtures. So called asymmetric synthesis has been a challenge for the synthetic chemist. Enantioselective synthesis is possible, proving optically pure intermediates are available. Such intermediates are in short supply and so synthesis of the racemic form, followed by chiral separation is still commonly used.
An overview of spirooxindole as a promising scaffold for novel drug discovery
Published in Expert Opinion on Drug Discovery, 2020
Li-Ming Zhou, Ren-Yu Qu, Guang-Fu Yang
With the growing reports of the extensive and excellent biological activities regarding the spirooxindole-based natural products and the analogs, the structural modification based on this subject also has captured much attention, which lays an abundant and solid material foundation for the exploration and discovery of pharmaceutical agents. Due to the existence of the chiral carbon atom of spirooxindole and its huge structural alterability, various derivatives can be constructed based on the structure of 2-oxindole via forming different kinds of the non-planar tricyclic or polycyclic scaffold at the C-3 site of oxindole. Its synthetic methods, especially the simple and high-efficiency asymmetric synthesis, have always been a hot field studied by researchers. Actually, numerous synthetic methods of spirooxindoles have been developed, which mainly include 1, 3-dipolar cycloaddition, domino Knoevenagel-Michael-cyclization, Michael-cyclization of isatins, C-H activation, and D-A reaction, etc. The related synthetic chemistry of spirooxindoles has been comprehensively summarized and described by organic chemists in the previous excellent reviews [25,201–212].
Fluorinated scaffolds for antimalarial drug discovery
Published in Expert Opinion on Drug Discovery, 2020
Charu Upadhyay, Monika Chaudhary, Ronaldo N. De Oliveira, Aniko Borbas, Prakasha Kempaiah, Poonam S, Brijesh Rathi
Fluorine also acts as an enabling agent for the process of self-disproportionation of enantiomers (SDE) [29,30]. SDE is a designed separation of non-racemic or scalemic mixture of compounds into enantioriched [31]. High polarization, hydrogen bonding and dipole-dipole interactions lead to the greater magnitude of SDE of the fluorinated compounds [32]. Eventually, fluorinated derivatives can be used as prototypes for analyzing the properties of SDE. However, asymmetric synthesis remains problematic for quaternary C-F stereogenic center [33].