Research Article

A Synthetic Strategy for Conjugation of Paromomycin to Cell-Penetrating Tat(48-60) for Delivery and Visualization into Leishmania Parasites

Scheme 2

Preparation of hydroxyl-protected paromomycin. Reagents and conditions: (i) Boc2O (15 equiv), Et3N (12 equiv), MeOH, H2O, 24 h, 60°C, 64%; (ii) Ac2O (16 equiv), anh. pyridine, DMAP, 20 h, R.T., 78%; (iii) TFA/CH2Cl2 (40%), 2 h, R.T., 100%.