Two main approaches aimed at the preparation of new pharmaceuticals using organosilicon compounds are now in vogue:

1 application of organosilicon compounds to prepare biologically active non-silicon-containing compounds;1 and

2 synthesis of organosilicon compounds possessing intrinsic biological activity.1 29

In the first case organosilicon compounds are used for the temporary protection of a functional group,1,17,27,30 as reagents mainly for reduction and cyana-tion,27 or as reaction intermediates facilitating the synthesis of the target nucleosides31 or ^-lactam antibiotics.32

The anti-cancer drug Tegafur (Ftorafur®, Futraful), 5-fluoro-1-(2-tetra-hydrofuryl)-2,4(1H,3H)-pyrimidinedione, was one of the first nucleoside analogues industrially prepared by the silyl method.31 The silylation converts the starting 5-fluorouracil into the more reactive liquid bis-silyl derivative. The reaction of this organosilicon intermediate with 2-chlorotetrahydrofuran already starts at —50 °C and proceeds smoothly at room temperature. The remaining protective group is easily removed by crystallization from alcohols.

Metallotherapeutic Drugs and Metal-Based Diagnostic Agents: The Use of Metals in Medicine Edited by Gielen and Tiekink © 2005 John Wiley & Sons, Ltd

In the second case the biological properties of organosilicon compounds themselves are exploited in drug design. There are three ways for obtaining biologically active derivatives of organosilicon compounds:

1 modification of biologically active organic compounds by introducing silicon-containing substituents;6,7,9,18,22,26

2 preparation of silicon analogues of known drugs by substitution of one or more carbon atoms for silicon atoms;6,7,10,14,15,19,22,25,28,29 and

3 synthesis and study of the biological activity of structurally specific organosilicon compounds lacking organic analogues.6,8,11,13,22,28,29

Using these methods several thousands of biologically active organosilicon compounds have been prepared; nine of them have entered human clinical trials, another four are used as agrochemicals.

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