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The synthetic route for key building blocks of rapalogs library
Reagents and conditions: a) 5 equiv allyl bromide, 2 equiv Cs2CO3, acetone, 2 h; b) 20% piperidine in DCM, 20 min; c) 1.5 equiv dihydro-4,4-dimethyl-2,3-furandione, 10% DMAP, Ar gas, toluene, reflux, overnight; d) DIC, Fmoc- amino acids (R2), 5% DMAP,1 h; e) 5% Pd(Ph3P)4, 3 equiv N-methylaniline, THF.
