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Reagents and conditions: (i) trimethylsilylacetylene, Pd2(PPh3)2, CuI, i-Pr2NH, THF, 70 °C; (ii) KF, MeOH/THF, rt, 69% for two steps; (iii) chloroacetyl chloride, K2CO3, THF, 0 °C, 5a (98%), 5b (84%), 5c (89%); (iv) NaN3, DMF, rt, 6a (97%), 6b (68%), 6c (95%); (v) CuSO4.5H2O, sodium ascorbate, AcOH, DMF/H2O, rt, 7a (32%), 7b (71%), 7c (41%). All detailed experimental procedures are provided in the Supplemental data.
