Drug synthesis natural product compounds

This series in heterocychc chemistry is being introduced to collectively make available critically and comprehensively reviewed hterature scattered in various journals as papers and review articles. All sorts of heterocyclic compounds originating from synthesis, natural products, marine products, insects, etc. will be covered. Several heterocyclic compounds play a significant role in maintaining life. Blood constituents hemoglobin and purines, as well as pyrimidines, are constituents of nucleic acid (DNA and RNA). Several amino acids, carbohydrates, vitamins, alkaloids, antibiotics, etc. are also heterocyclic compounds that are essential for life. Heterocyclic compounds are widely used in clinical practice as drugs, but all applications of heterocyclic medicines can not be discussed in detail. In addition to such applications, heterocyclic compounds also find several applications in the plastics industry, in photography as sensitizers and developers, and the in dye industry as dyes, etc. 

Breinbauer RP, Vetter IR, Waldmann H. (2002) From protein domains to drug candidates — natural products as guiding principles in the design and synthesis of compound libraries. Angew Chem Int Ed 41 2878-2890. 

Henderson WR Jr, Chi EY, Teo JL, Nguyen C, Kahn M. A Small Molecule Inhibitor of Redox-Regulated NF-(kappa B and Activator Protein-1 Transcription Blocks Allergic Airway Inflammation in a Mouse Asthma Model. J. Immunol. 2002 169 5294-5299. Breinbauer R, Vetter IR, Waldmann H. From protein domains to drug candidates-natural products as guiding principles in the design and synthesis of compound libraries. Angew. Chem., Int. Ed. Eng. 2002 41 2879-2890. 

Figure 6.26 Principal component analysis of chemical space properties for groups of compounds categorized as drugs, bioactives, natural products, fragments, diversity oriented synthesis (DOS) and Rule-of-Five. Numbered compounds representative of the various categories are given in the reference. (Reprinted with permission from Shelat, A. A., Guy, R.K. The interdependence between screening methods and screening libraries. Curr. Opin. Chem. Biol. 2007, 11, 244-251, copyright 2007, Elsevier.)...

From conventional reaction conditions to microwave-assisted catalytic transformations of various substrates 13COC448, 13COC457. Microwave-aided synthesis of organic compounds including drugs and natural products 12AJC1647. 

The first method using the j-BuLi-sparteine aggregate was successfully applied to the asymmetric protonation of 2-(l-phenylethyl)pyridine 5 to afford (S)-5 in good yield with 50% ee. The 4-aryl-tetrahydroisoquinoline backbone 6, which is of considerable interest because of its presence in several natural or bioactive products such as sertraline or nomifensine, was obtained in good yield with 88% ee. Although the backbone of bioactive compounds was synthesized in an asymmetric fashion, the total synthesis of the corresponding drugs or natural products has not yet been achieved to date. 

Drugs of particularly complex structure are often prepared commercially by partial synthesis from some abundant, structurally related, natural product obtained from plants. The majority i)f steroid drugs are in fact prepared in just this way. Prostaglandins are unique in that no prostanoid compounds have yet been found in plants, a perhaps surprising finding in view of the wide distribution of essential fatty acids in plant materials. 

---