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    REGIO-SELECTIVE SYNTHESIS OF IMIDAZO[1,2-a]PYRIMIDINES
    1.
    发明申请
    REGIO-SELECTIVE SYNTHESIS OF IMIDAZO[1,2-a]PYRIMIDINES 审中-公开

    公开(公告)号：US20200369670A1

    公开(公告)日：2020-11-26

    申请号：US16869512

    申请日：2020-05-07

    Applicant: Genentech, Inc.

    Inventor： Kyle Bradley Pascual Clagg ,  Nicholas Andrew White ,  Haiming Zhang ,  Francis Gosselin ,  William Nack ,  Paul D. O'Shea

    IPC: C07D487/04 ,  C07F9/24

    Abstract: A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb) comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2 This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.

    Regio-selective synthesis of imidazo[1,2-a]pyrimidines
    4.
    发明授权
    Regio-selective synthesis of imidazo[1,2-a]pyrimidines 有权

    公开(公告)号：US11325912B2

    公开(公告)日：2022-05-10

    申请号：US16869512

    申请日：2020-05-07

    Applicant: Genentech, Inc.

    Inventor： Kyle Bradley Pascual Clagg ,  Nicholas Andrew White ,  Haiming Zhang ,  Francis Gosselin ,  William Nack ,  Paul D. O'Shea

    IPC: C07D487/04 ,  C07F9/24

    Abstract: A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb) comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2 This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.

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