Synthesis of boronated 1-aminocyclobutanecarboxylic acids : sources of potential Boron Neutron Capture Therapy Agents

The syntheses of several boronated 1-amino cyclobutanecarboxylic acids (ACBC) were achieved. These compounds were synthesized as potential Boron Neutron CaptureTherapy (BNCT) Agents. The first derivative synthesized was w-carboranyl ACBC.This compound failed to show the desirable properties that a BNCT agent must have.This led the investigator to explore another group of compounds. The second set of derivatives synthesized was a series of 4-dihydroxyborylphenyl analogs of 1-aminocyclobutanecarboxylic acid. The number of carbon spacers (as methylene units)was varied between the cyclobutane ring and the aromatic ring to introduce different degrees of lipophilicily into the molecule. Fom compounds with 0,2,3 and 7 methylene spacers were synthesized and are awaiting evaluation as Boron Neutron Capture Therapy Agents

Phosphine-free palladium-catalyzed direct arylation of imidazo[1,2-a]pyridines with aryl bromides at low catalyst loading.

International audienceLigand-free Pd(OAc)(2) was found to catalyze very efficiently the direct arylation of imidazo[1,2-a]pyridines at C3 under very low catalyst concentration. The reaction can be performed employing as little as 0.1-0.01 mol % catalyst with electron-deficient and some electron-excessive aryl bromides