Synthesis through selective activation

Figure 7. DALA synthesis through selective activation of C5 in levuiinic acid...

Today, the application of hypervalent iodine reagents still dominates the reaction landscape of electrophilic N-atom transfer processes, a testament to the unique reactivity of such oxidants. Nevertheless, the past decade has witnessed a flurry of activity aimed at the invention of new reagents and protocols that enable amine and amine derivative synthesis through selective C-H bond modification. We have attempted to highlight many of these recent discoveries, with apologies in advance... 

SCHEME 6.36 Mong s one-pot synthesis of trisaccharide 180 through combination of selective activation and armed-disarmed approach. 

Pizzarello S, Weber AL (2010) Stereoselective syntheses of pentose sugars under realistic prebiotic conditions. Orig Life Evol Biosph 40 3-10 Powner MW, Garland B, Sutherland JD (2009) Synthesis of activated pyrimidine ribonucleotides in prebiotically plausible conditions. Nature 459 239-242 Scumlimbrene BR, Miller SJ (2001) Discovery of a catalytic asymmetric phosphorylation through selection of a minimal kinase mimic a concise total synthesis of D-myo-inositol-phosphate. J Am Chem Soc 123 10125-10126... 

The bioactive conformation is consistent with the farmacoforic points that are identified through structure activity relationship studies (SAR). SAR studies include the synthesis of many peptide and/or non peptide analogues displaying selectivity for one or another of the receptors and their pharmacologically defined subtypes [19] such as delta 1- and delta2-opioid receprtor subtypes [20]. 

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