Process for preparation of chiral 3-aminopyrrolidine and analogous bicyclic compounds

    公开(公告)号:AU7300498A

    公开(公告)日:1998-06-10

    申请号:AU7300498

    申请日:1997-11-18

    Applicant: ABBOTT LAB

    Abstract: A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof, optional additional substitution closing of the second ring, and hydrogenolysis to remove a ring-nitrogen protecting group.

    COMPUESTO DERIVADO DE PIRROL SUSTITUIDO, COMPOSICION FARMACEUTICA Y SU USO EN LA FABRICACION DE UN MEDICAMENTO PARA INHIBIR LA FARNESILTRANSFERASA

    公开(公告)号:AR035375A1

    公开(公告)日:2004-05-12

    申请号:ARP010105568

    申请日:2001-11-29

    Applicant: ABBOTT LAB

    Abstract: Un compuesto derivado de pirrol sustituido de fórmula (1) o una sal aceptable para uso terapéutico del mismo, donde E es un anillo carbocíclico aromático o no aromático de cinco, seis o siete miembros donde entre cero y tres átomos de carbono están reemplazados por nitrógeno; F y G son independientemente seleccionados del grupo formado por C y N; con la salvedad de que cuando uno de F y G es N, el otro es C; L1 y L2 son cada uno independientemente seleccionados del grupo formado por un enlace C2 alquileno, C2 alquinileno, O, NR9, C(O), S, S(O). SO2, SO2NR9, NR9SO2, C(O)NR9, NR9C(O), y CO2; X se selecciona entre el grupo formado por S y NR7; R1 se selecciona entre en grupo formado por arilo, arilalquilo, heterociclo, y (heterociclo)alquilo; R2 se selecciona entre el grupo formado por hidrógeno, alcoxi, alquilo, amino, aminoalquilo, ciano, cianoalquilo, cicloalquilo, cicloalquilalquilo, halo, haloalquilo, heterociclo, (heterociclo)alquilo, hidroxilo, e hidroxialquilo; R3 se selecciona entre el grupo formado por arilo, heterociclo y cicloalquil; R4-6 son cada uno independientemente seleccionado del grupo formado por hidrógeno NR9C(O), C(O)NR9, alcanoilo, alquenilo, alcoxi, alcoxialquilo, alquilo, alquilsulfonilo, alquinilo, amido, amino, aminoalquilo, aminosulfonilo, arilo, arilalquilo, ariloxi, arilsulfonilo; azido, carboxi, ciano, cianoalquilo, cicloalquilo, cicloalquilalquilo, halo, haloalcoxi, haloalquilo, heterociclo, (heterociclo)alquilo, hidroxilo, hidroxialquilo, nitro, nitroalquilo, oxo, y tio(oxo); R7 se selecciona entre el grupo formado por hidrógeno, alquilo, arilo, cicloalquilo, cicloalquilalquilo, heterociclo (heterociclo)alquilo, y trialquilsililo; R9 se selecciona entre el grupo formado por hidrógeno, alcoxialquilo, alquil, amidoalquilo, aminoalquilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, carboxialquilo, heterociclo (heterociclo), alquilo, hidroxialquilo, y un grupo protector de nitrógeno; cada R12 se selecciona independientemente del grupo formado por hidrógeno, alcoxi, alquilo, amino, halo e hidroxilo; m es 0, 1, 2, 3, o 4; n es 0, 1, 2, 3 o 4; p es 0, 1, 2, 3 o 4; y q es 0, 1, 2, 3, o 4. También se revelan composiciones inhibidoras de la farnesiltransferasa y el uso de dichos compuestos en la fabricación de medicamentos para inhibir la farnesiltransferasa en un paciente.

    23.
    发明专利
    未知

    公开(公告)号:DE69802274T2

    公开(公告)日:2002-07-18

    申请号:DE69802274

    申请日:1998-02-06

    Applicant: ABBOTT LAB

    Abstract: A process for the preparation of a compound having the formula: wherein R1, R2, R3, R4, and R5 are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.

    24.
    发明专利
    未知

    公开(公告)号:PT971919E

    公开(公告)日:2002-04-29

    申请号:PT98904979

    申请日:1998-02-06

    Applicant: ABBOTT LAB

    Abstract: A process for the preparation of a compound having the formula: wherein R1, R2, R3, R4, and R5 are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.

    25.
    发明专利
    未知

    公开(公告)号:DK0971919T3

    公开(公告)日:2002-01-28

    申请号:DK98904979

    申请日:1998-02-06

    Applicant: ABBOTT LAB

    Abstract: A process for the preparation of a compound having the formula: wherein R1, R2, R3, R4, and R5 are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.

    26.
    发明专利
    未知

    公开(公告)号:DE69802274D1

    公开(公告)日:2001-12-06

    申请号:DE69802274

    申请日:1998-02-06

    Applicant: ABBOTT LAB

    Abstract: A process for the preparation of a compound having the formula: wherein R1, R2, R3, R4, and R5 are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.

    28.
    发明专利
    未知

    公开(公告)号:AT207920T

    公开(公告)日:2001-11-15

    申请号:AT98904979

    申请日:1998-02-06

    Applicant: ABBOTT LAB

    Abstract: A process for the preparation of a compound having the formula: wherein R1, R2, R3, R4, and R5 are defined, from an enamine by chain expansion and ring closure followed by additional derivatization, treatment with a 3-alkoxyl-acryloyl compound, another ring closure, and converting a hydroxyl group to a leaving group.

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