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Formation of key dipole (a) and acyclic (b) starting materials: (i) 11 (1.0 equiv.), NH2OH (2.0 equiv.), EtOH, r.t., 10 min; then NCS (1.1 equiv.), DMF, r.t., 0.5 h, 99 %; (ii) 12 (1.0 equiv.), NEt3 (1.0 equiv.), DCE, 0 °C, 3 min, used immediately; (iii) 14 (1.0 equiv.), Boc2O (0.95 equiv.), K2CO3 (1.5 equiv.), EtOAc, H2O, r.t., 12 h, 93 %; (iv) 15 (1.0 equiv.), MsCl (1.25 equiv.), NEt3 (3.0 equiv.), DCM, –15 °C ‐ r.t., 2 h, 94 %.
