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Reagents and conditions: (i) Savinase, 1,4-butanediol, pH 8, 27%; (ii) CBZThr (O-tBu)-Dap(BOC)OH, HATU, NEtiPr2, DCM, quant.; (iii) PhB(OH)2, Pd(OAc)2, X-Phos, K3PO4,toluene, 100°C, 50%; (iv) NH3+HCOO-, 10% Pd/C, MeOH; 93%; (v) RCO2H (N-BOC protected), HATU, NEtiPr2, DCM, DMF; (vi) TFA, DCM, followed by prep HPLC, 23% over 2 steps.
