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    PREPARATION OF OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES
    23.
    发明专利
    PREPARATION OF OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES 未知

    公开(公告)号：NZ595275A

    公开(公告)日：2013-07-26

    申请号：NZ59527507

    申请日：2007-02-16

    Applicant: ABBOTT LAB

    Inventor： ZHENG GUO ZHU ,  GREGG ROBERT J ,  ZHANG GEOFF G

    IPC: C07D487/04 ,  A61K31/407 ,  A61K31/501 ,  C07D237/14

    Abstract: 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.

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