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    Process for preparing azabicyclic compounds
    3.
    发明专利
    Process for preparing azabicyclic compounds 未知

    公开(公告)号：NZ598277A

    公开(公告)日：2014-03-28

    申请号：NZ59827710

    申请日：2010-09-17

    Applicant: VERTEX PHARMA

    Inventor： AMBHAIKAR NARENDRA BHALCHANDRA ,  HUGHES ROBERT ,  BEAR BRIAN RICHARD ,  FANNING LEV T D ,  LITTLER BENJAMIN

    IPC: C07D487/08

    Abstract: 598277 The present disclosure relates to a process for preparing azabicyclic compounds that are useful intermediates for synthesizing pharmaceutical compounds or salts thereof. The process comprises contacting trans-4-aminocyclohexanol with Boc anhydride to produce a compound of formula A, contacting a compound of formula A with methanesulfonic acid to produce a compound of formula B contacting a compound of formula B with trifluoroacetic acid to produce a compound of formula C and contacting a compound of formula C with hydroxide to produce a compound of formula 7.

    Proceso para preparar compuestos azabicíclicos
    9.
    发明专利
    Proceso para preparar compuestos azabicíclicos 未知

    公开(公告)号：ES2540810T3

    公开(公告)日：2015-07-13

    申请号：ES10757544

    申请日：2010-09-17

    Applicant: VERTEX PHARMA

    Inventor： AMBHAIKAR NARENDRA BHALCHANDRA ,  BEAR BRIAN RICHARD ,  FANNING LEV T D ,  HUGHES ROBERT ,  LITTLER BENJAMIN

    IPC: C07D487/08

    Abstract: Un proceso para preparar el Compuesto 7.**Fórmula** o una sal farmacéuticamente aceptable del mismo, que comprende poner en contacto trans-4-aminociclohexanol con anhídrido Boc para producir un compuesto de fórmula A**Fórmula** poner en contacto un compuesto de fórmula A con cloruro de metanosulfonilo para producir un compuesto de fórmula B**Fórmula** poner en contacto un compuesto de fórmula B con ácido trifluoroacético para producir un compuesto de fórmula C**Fórmula** y poner en contacto un compuesto de fórmula C con hidróxido para producir un compuesto de fórmula 7.

    Process for preparing modulators of cystic fibrosis transmembrane conductance regulator
    10.
    发明专利
    Process for preparing modulators of cystic fibrosis transmembrane conductance regulator 未知

    公开(公告)号：NZ600172A

    公开(公告)日：2014-07-25

    申请号：NZ60017210

    申请日：2010-10-21

    Applicant: VERTEX PHARMA

    Inventor： AMBHAIKAR NARENDRA BHALCHANDRA ,  HUGHES ROBERT ,  HURLEY DENNIS JAMES ,  LEE ELAINE CHUNGMIN ,  LITTLER BENJAMIN ,  NUMA MEHDI ,  ROEPER STEFANIE ,  SHETH URVI

    IPC: C07D215/56 ,  C07D487/08

    Abstract: Disclosed herein is a process for producing the hydrochloride salt of Compound 1 having solid Form A-HCl comprising: (a) reacting Compound 2 with the hydrochloride salt of Formula 3 (3-HCl) in the presence of a coupling agent, a base, and a polar aprotic solvent; wherein the coupling agent is selected from the group consisting of 2-chloro-1,3-dimethyl-2-imidazolium tetrafluoroborate, 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (HBTU), 2-chloro-4,6-dimethoxy-1,3,5-triazine, 1-H-benzotriazolium-1-[bis(dimethyl amino)methylene]-5-chlorohexafluorophosphate (HCTU), 2-(1H-7-Azabenzotriazol-1-yl)-1,1,3,3-tetramethyl uronium hexafluorophosphate (RA TU), 1-hydroxybenzotriazole (HOBT)/ 1-(3-(dimethylamino)propyl)-3-ethyl-carbodiimide hydrochloride (EDCl), and propane phosphonic anhydride; wherein the base is selected from the group consisting of K2CO3, Et3N, N-methylmorpholine (NMM), pyridine, and diisopropylethyl amine (DIEA); and wherein the polar aprotic solvent is selected from the group consisting of ethyl acetate, isopropyl acetate, tetrahydrofuran, methylethyl ketone, N-Methyl-2-pyrrolidone, acetonitrile, N,N-dimethyl formamide, and 2- methyltetrahydrofuran; and (b) treating a mixture comprising the product of step (a) with HCl; wherein step (a) is performed at a reaction temperature that is maintained between 15°C and 70°C.

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