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    Un procedimiento para la preparación del promotor de la apoptosis ABT-263
    5.
    发明专利
    Un procedimiento para la preparación del promotor de la apoptosis ABT-263 未知

    公开(公告)号：ES2409263T3

    公开(公告)日：2013-06-26

    申请号：ES09767695

    申请日：2009-06-18

    Applicant: ABBOTT LAB

    Inventor： FRANCZYK THADDEUS ,  HILL DAVID ,  HAIGHT ANTHONY ,  MCLAUGLIN MAUREEN ,  SHEKHAR SHASHANK ,  YU SU ,  MEI JIANZHANG ,  WANG LEI

    IPC: C07D295/13 ,  C07D295/155

    Abstract: Un procedimiento para elaborar N-(4-(4-((2-(4-clorofenil)-5,5-dimetil-1-ciclohex-1-en-1-il)metil)piperazin-1-il)benzoil)-4-(((1R)-3-(morfolin-4-il)-1-((fenilsulfanil)metil)propil)amino)-3-((trifluorometil)sulfonil)bencenosulfonamida,o una de sus sales farmacéuticamente aceptables, que comprende: (e) hacer reaccionar el 2-(4-clorofenil)-5,5-dimetilciclohex-1-eno-1-carbaldehído, 4-piperazin-1-ilbenzoato de etilo yun primer agente reductor y aislar o no aislar el 4-(4-((2-(4-clorofenil)-5,5-dimetilciclohex-1-en-1-il)metil)piperazin-1-il)benzoato de etilo; (f) hacer reaccionar el 4-(4-((2-(4-clorofenil)-5,5-dimetilciclohex-1-en-1-il)metil)piperazin-1-il)benzoato de etilo y unatercera base acuosa, y aislar o no aislar el ácido 4-(4-((2-(4-clorofenil)-5,5-dimetilciclohex-1-en-1-il)metil)piperazin-1-il)benzoico; y (g) hacer reaccionar el ácido 4-(4-((2-(4-clorofenil)-5,5-dimetilciclohex-1-en-1-il)metil)piperazin-1-il)benzoico, 4-(((1R)-3-morfolin-4-il-1-((feniltio)metil)propil)amino)-3-((trifluorometil)sulfonil)bencenosulfonamida y un primer reactivo deacoplamiento con o sin una cuarta base y con o sin un reactivo de acoplamiento auxiliar, y aislar o no aislar la N-(4-(4-((2-(4-clorofenil)-4,5-dimetil-1-ciclohex-1-en-1-il)metil)piperazin-1-il)benzoil)-4-(((1R)-3-(morfolin-4-il)-1-((fenilsulfanil)metil)propil)amino)-3-((trifluorometil)sulfonil)bencenosulfionamida.

    A PROCESS FOR THE PREPARATION OF THE APOPTOSIS PROMOTER ABT-263
    6.
    发明专利
    A PROCESS FOR THE PREPARATION OF THE APOPTOSIS PROMOTER ABT-263 未知

    公开(公告)号：NZ589732A

    公开(公告)日：2012-08-31

    申请号：NZ58973209

    申请日：2009-06-18

    Applicant: ABBOTT LAB

    Inventor： FRANCZYK THADDEUS S ,  HILL DAVID R ,  HAIGHT ANTHONY R ,  MCLAUGLIN MAUREEN ANN ,  SHEKHAR SHASHANK ,  YU SU ,  MEI JIANZHANG ,  WANG LEI

    IPC: C07D295/155 ,  C07D295/023

    Abstract: Disclosed A process for making ABT-263 (7) an apoptosis promoter having the proper chemical name: N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide, comprising: (a) reacting 4,4-dimethylcyclohexanone, an alkyl formate and a first base to provide (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone and isolating or not isolating the (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone; (b) reacting the (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone, a second base and a first silyl ether protecting group reagent to provide a first protected (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone and isolating or not isolating the first protected (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone; (c) reacting the first protected (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone and 4-chlorophenyl magnesium bromide to provide the first protected (2E)-1-(4-chlorophenyl)-2-(hydroxymethylene)-4,4-dimethylcyclohexanol; and isolating or not isolating the first protected (2E)-1-(4-chlorophenyl)-2-(hydroxymethylene)4,4-dimethylcyclohexanol; and (d) reacting the first protected (2E)-1-(4-chlorophenyl)-2-(hydroxymethylene)-4,4-dimethylcyclohexanol and a first acid to provide 2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-ene-1-carbaldehyde and isolating or not isolating the 2-(4-chlorophenyl)5,5-dimethylcyclohex-1-ene-1-carbaldehyde; (e) reacting 2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-ene-1-carbaldehyde, ethyl 4-piperazin-1-ylbenzoate and a first reducing agent and isolating or not isolating the ethyl 4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoate; (f) reacting ethyl 4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoate and an aqueous third base, and isolating or not isolating the 4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoic acid; and (g) reacting 4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoic acid, 4-(((1R)-3-morpholin-4-yl-1-((phenylthio)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide, a first coupling reagent, and, optionally; a first auxiliary coupling reagent and isolating or not isolating the N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1- ((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide.

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