Design, synthesis and biological evaluation N2-(2-alkyoxy-6-aliphatic aminopyridin-3-yl)-2,4-diaminepyrimidine derivatives bearing acylamino or DBTD ‘head’ as potential ALK inhibitors

Fragment-based drug discovery: opportunities for organic synthesis

“…As a representative example, the dihydrobenzothiazine-dioxide ( 10) is poorly socialised when analysed by the fragment network. 84 However, 'simplification' to the reduced dihydrobenzothiazine (11) results in identification of several commercially available analogues. 85 It is important to note that synthetic elaboration of every carbon position of 11 is exemplified thus enabling access to every growth vector of 10 through a single-synthetic transformation step.…”