Use of Green Solvents in Metallaphotoredox Cross-Electrophile Coupling Reactions Utilizing a Lipophilic Modified Dual Ir/Ni Catalyst System.

Facilitating photoredox coupling reactions in process-friendly green solvents was achieved by the successful application of a dual Ir/Ni catalyst system with enhanced solubility properties. These photochemical reactions (specifically Br-Br sp2-sp3 cross electrophile coupling) are reported in a head to head comparison to the standard di-t-Bu bipyridine ligand Ir/Ni catalyst system. This presentation highlights the benefits of altering the solubility properties of the ligands used in the Ir/Ni dual catalyst.

AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey.

A series of 11-oxa prostaglandin analogs was evaluated for FP receptor binding and activation. Several compounds having aryloxy-terminated lower chains were found to be potent agonists. Topical ocular dosing of AL-12182, the isopropyl ester prodrug of the potent agonist 13, lowered intraocular pressure in the monkey by 40% accompanied by minimal conjunctival hyperemia in the rabbit. AL-12182 was synthesized on multigram scale starting with D-sorbitol.