- Section G Revealed Synoptic Question 15 Answer Both Parts Of This Question Drugs A And B Figure Q15a Are Topoisome 1 (92.53 KiB) Viewed 25 times
15. Answer BOTH parts of this question:
Drugs A and B (Figure Q15a) are topoisomerase inhibitors and
anticancer agents.
(a) Aside from their inhibitory activity, briefly describe five
other types of study
or data that a medicinal chemist could use in order to rank these
different
chemical series?
SECTION G (revealed synoptic question) 15. Answer BOTH parts of this question: Drugs A and B (Figure Q15a) are topoisomerase inhibitors and anticancer agents. (a) Aside from their inhibitory activity, briefly describe five other types of study or data that a medicinal chemist could use in order to rank these different chemical series? НО. H HO Drug A Drug B Figure Q15a (15 marks) (b) Your company is interested in synthesizing a new drug intermediate: NOZ Eto New drug intermediate (i) With the use of appropriate diagrams, draw a fully labelled, multistep retrosynthesis of the new intermediate. Your scheme must lead back to CH3CH2CO2Et and meta-NO2-PhCH2Br (1-bromomethyl-3- nitrobenzene). (8 marks) (ii) Suggest a further retrosynthesis of meta-NO2-PhCH2Br, leading back to benzene. (2 marks) Your answers should include any required disconnections, retrosynthetic arrows, functional group interconversions, synthons and synthetic equivalents. If necessary, comment on any possible selectivity problems. (Total = 25 marks)