A DNA Encoded Library (DEL) generated the hit compound 4 which was found to show potent CGRP inhibition. The library was

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A Dna Encoded Library Del Generated The Hit Compound 4 Which Was Found To Show Potent Cgrp Inhibition The Library Was 1 (60.3 KiB) Viewed 6 times

A Dna Encoded Library Del Generated The Hit Compound 4 Which Was Found To Show Potent Cgrp Inhibition The Library Was 2 (142.03 KiB) Viewed 6 times

A DNA Encoded Library (DEL) generated the hit compound 4 which was found to show potent CGRP inhibition. The library was generated from the DNA supported building block 3, and the benzimidazole core was prepared by the mild oxidative condensation reaction highlighted below: MeN F NO2 DO OH H2N. 3 N 4 Benzimidazole synthesis: R R NH ArCHO Na S205 Ar N NH2

(0) Devise a synthetic sequence that would transform 3 into a DNA-supported analogue of compound 4 (i.e. a derivative of 4 where ‘NHż is replaced by ‘NH-DNA'.) [3 marks] 4 (ii) With the aim of generating a DEL using your synthetic sequence, indicate which cycles allow the introduction of multiple molecular scaffolds. [2 marks] (iii) By carrying out a search of commercially available compounds on SciFinder Scholar, state how many molecular scaffolds you expect to use at each of the cycles where a range of molecular scaffolds are introduced. You should clearly show the molecular structure that you used in your search, and justify why you chose it. (10 marks] (iv) Based on your answers to (i)-(iii), state how many compounds you expect to generate in your DEL.