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Reagents and conditions: (a) Benzyl isocyanide, N-Boc-4-piperidinone, acetonitrile/methanol (4:1), 65 °C, 24 h; (b) 55% TFA/DCM; (c) Acid, DIC, HOBt, DMF, r.t., overnight or Sulfonyl chloride/isocyanate/thioisocyanate, DIEA, DMF, r.t., overnight; (d) HF cleavage, 0 °C, 1.5 h.
