Organic Synthesis in Drug Discovery and Development

Chirality of NDEs is crucial because of the three-dimensional nature of biological target molecules and 68% of the top 200 marketed drugs are optically pure. Consequently, the stereoselective approach to drug molecules will remain important for many years to come. 

An NDE is expected to meet an unmet medical need or to improve therapy where existing drugs have proved ineffective due to lack of efficacy, development of resistance or tolerance, to unexpected toxic side-effects, or have shown incompatibility with other drags. New pathological states or diseases are also being continuously revealed and require effective therapy. 

In the next three sections, we briefly present some characteristics of the R D process in the pharmaceutical industry and the specific approaches that are being taken to confront the scientific and organizational problems. 

To provide background information for the role of synthetic chemistry, some aspects of the R D process in innovative pharmaceutical companies deserve comment. The complexity of the usual multidisciplinary research process in developing an NDE is presented schematically in Fig. 1.1. 

The organizational and value chain in pharmaceutical R D requires that a wide range of activities are interconnected, some of them loosely, the others strongly integrated. Individuals prepared to champion this progression are crucial, and they are recruited from among the scientists and physicians involved. 

---

These scientists qualifications surpass what M.S. chemists offer. In summary, doctorate-level chemists demonstrate mastery of organic chemistry and proficiency in synthesis if they find employment in drug discovery or development research. Their dissertations present substantial pieces of original and successful research. Scientific publications, patent inventorships, and postdoctoral research experiences represent bonuses to any employer. 

Biel, J. H., Martin, Y. C. Organic synthesis as a source of new drugs. In Drug Discovery-Science and Development in a Changing Society (Society, A. C., Ed.). American Chemical Society Washington, DC, 1971, Vol. 108, pp. 81-111. 

---