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Abstract 1H-Benzotriazole has found wide applicability as a highly effective synthetic auxiliary in solution and solid phase reactions. The aim of this study was to develop practical synthetic routes of potential importance for the construction of pharmaceutically important structural motifs and compounds of biological interest utilizing N-acylbenzotriazoles. In addition, the design, synthesis and biological evaluation of novel anti-HIV drug candidates is also discussed. The thesis is presented in six parts; Chapter 1 starts with description of the common use of benzotriazole as a synthetic auxillary and then, concentrates on the use of N-acyl benzotriazoles as advantageous alternatives to acid chlorides and other coupling reagents. Subsequently, chapter 1 deals with the useful synthesis of azo dye labeled sugars terpenes and steroids using N-acyl benzotriazoles in the presence of DBU. Chapter 2 illustrates the selective N- and S-acylation of cysteine using N-acylbenzotriazoles in basic and neutral medium respectively. Chapter 3 describes the selective synthesis of N- and S-acyl glutathiones using N-acyl and N-(-aminoacyl)benzotriazole and outline the difference between the acylation of cysteine and glutathione. Chapter 4 presents efficient method for the synthesis of di- and tripeptide alcohols through selective acylation of the amino group of -aminoalcohols with N-(-aminoacylbenzotriazoles and N-(-dipeptidoy)benzotriazoles |