Scheme 3a.

a (a) Boc2O, cat. DMAP, THF, rt, 16 h, 99%; (b) H2, 10% Pd/C, EtOH, rt, 16 h, 100%; (c) N-(2-pyrimidinyl)-4-hydroxymethylpiperidine, PPh3, DIAD, THF, rt, 16 h; (d) TFA/CH2Cl2, 1:1, rt, 3 h, 92% (two steps).

a (a) Boc2O, cat. DMAP, THF, rt, 16 h, 99%; (b) H2, 10% Pd/C, EtOH, rt, 16 h, 100%; (c) N-(2-pyrimidinyl)-4-hydroxymethylpiperidine, PPh3, DIAD, THF, rt, 16 h; (d) TFA/CH2Cl2, 1:1, rt, 3 h, 92% (two steps).