aReagents: (i) Me(OMe)NH·HCl, EDCI, HOBT, Et3N, DCM; (ii) MeMgBr, THF; (iii) Br2, HOAc/HBr; (iv) 3-methylphenylthiourea 118, EtOH; (v) H2, Pd/C, EtOH; (vi) Ac2O, dioxane; (vii) PdCl2(PPh3)2, CuI, TMSC≡CH, Et3N, DMF, then TBAF; (ix) PdCl2(PPh3)2, CuI, HC≡CCH2OH, Et3N, DMF; (x) PdCl2(PPh3)2, CuI, HC≡CCH2OMe, Et3N, DMF; (xi) PdCl2dppf, K2CO3, CH3COPhB(OH)2, toluene, EtOH, H2O, DMF. $ = commercially available.