“…To understand the structure–activity relationships (SAR) and to develop drug candidates as well as probes for investigating the translation process, many efforts have been given to the chemical synthesis of puromycin and hygromycin A derivatives. − Especially, the total synthesis of hygromycin A has been achieved by Ogawa et al in 1989 and by Donohoe et al in 2009, respectively, , and a synthesis of the 1,2- trans -furanoside analogue of hygromycin A was accomplished by Trost et al In contrast, study toward the synthesis of A201A, which demands incorporation/elaboration of the unique hexofuranose D unit with an exocyclic enol ether moiety, has never been reported. Here, we communicate the first synthesis of this complex nucleoside antibiotic ( 1 ).…”