Abstract - 595275 Disclosed is a process of preparing compounds of formula (IV), wherein R1 is an alkyl group and Cy1a is aryl or heteroaryl, comprising the step of treating a compound of formula (III) with alkylating conditions to provide a compound of formula (IV). Also disclosed is a process for preparing a compound of formula (IV), wherein R1 is an alkyl group, and Cy1 is aryl, comprising the steps of: a) providing ethyl (3aR,6aR)-hexahydropyrrolo[2,3-c]pyrrole-5(1H)-carboxylate dibenzoyl-D-tartrate salt b) treating ethyl (3aR,6aR)-hexahydropyrrolo[2,3-c]pyrrole-5(1H)-carboxylate dibenzoyl-D-tartrate salt with a base to yield a compound of formula (IIIa) c) heating the compound of formula (IIIa), wherein P is ethoxycarbonyl and a compound of formula (IIIb), with a carbonate base, a palladium source, and Xantphos in a solvent, to provide a compound of formula (IIIc) d) heating the compound of formula (IIIc) with a compound of formula (IIId), a carbonate base and a copper source in a high-boiling polar solvent (such as dimethylformamide (DMF), dimethylacetamide (DMA), pyridine, or 4-methylpyridine) to provide a compound of formula (IIIe) e) removing the ethoxycarbonyl group to provide a compound of formula (III), and alkylating the compound of formula (III) to provide a compound of formula (IV), wherein the compound of formula (IV) is a compound such as 2-{ 4-[(3aR,6aR)-5-methylhexahydropyrrolo[3,4-b]pyrrol-1(2H)-yl]-1,1-biphenyl-4-yl} pyridazin-3(2H)one.
