Elegant and Cost-Effective Synthetic Design

The heart of synthesis is in the design of the synthetic scheme for the given target molecule. All the technological advances (discussed above) can only supplement the synthetic scheme. Innovation, elegance, and brevity in the synthetic design are essential 

Richard Willstatter achieved the first synthesis of tropinone in 1901 (see Fig. 2.4). At that time, structure determination was not always equivocal, and final proof could only be established by unambiguous synthesis of the compound with the suspected structure followed by comparison with an authentic sample of the natural product. Thus, synthesis was often a matter of utilitarian necessity rather than the creative, elegant art form illustrated by the work of many of the great synthetic chemists such as Woodward and Corey. 

In fact, we can view this synthesis of tropinone as one of the earliest examples oi multicomponent reactions (MCR). MCRs are convergent reactions in which three or more starting materials react to form a product, where basically all or most of the atoms contribute to the newly formed product. In an MCR, a product is assembled according to a cascade of elementary chemical 

Name of the Reaction Reactants/ Components Predominant Product 

BiginelU Carbonyl compounds + esters + amines Diazine derivatives 

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