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. Author manuscript; available in PMC: 2016 Jan 29.
Published in final edited form as: J Med Chem. 2016 Jan 13;59(2):592–608. doi: 10.1021/acs.jmedchem.5b01369

Scheme 1. Preparation of diamidines 4a-c.

Scheme 1

Reagents and conditions: (a) CsCO3, acetone, reflux, 14 hrs.; (b) methanol:dioxane (1:1), HCl gas; (c) ethanolic ammonia, ammonium chloride, 80 °C, 32 hrs. Cyclic amidines (5a-d, 6a-d, and 7a-d) were synthesized according to literature with some modification (Scheme 2). Specifically, treatment of dibenzimidate with diaminoethane, diaminopropane and diaminobutane at room temperature in DMF accomplished cyclic amidine in satisfactory yield31-33. Increasing the chain length of the diamine results in open chain products (8 and 9a, 9b), which were useful for testing aliphatic chain derivatives of varying lengths (Scheme 2).