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AR076897A1 - Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos - Google Patents

Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos

Info

Publication number
AR076897A1
AR076897A1 ARP100101869A AR076897A1 AR 076897 A1 AR076897 A1 AR 076897A1 AR P100101869 A ARP100101869 A AR P100101869A AR 076897 A1 AR076897 A1 AR 076897A1
Authority
AR
Argentina
Prior art keywords
compound
produce
order
organic solvent
produce compound
Prior art date
Application number
Other languages
English (en)
Inventor
David A Siesel
Original Assignee
Vertex Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of AR076897A1 publication Critical patent/AR076897A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Un proceso para la provision del acido 3-(6-(1-(2,2-difluorbenzo[d]1,3]dioxol-5-il) ciclopropanocarboxamido)-3-metilpiridin-2-il)benzoico en forma sustancialmente libre. Reivindicacion 1: Un proceso para la preparacion de Compuesto (1): que comprende las etapas de: i) la provision de 2-bromo-3-metilpiridina Compuesto (2) y ácido 3-(t-butoxicarbonil)fenilboronico Compuesto (3); ii) el acoplamiento cruzado de compuesto 2 y compuesto 3 en una mezcla bifásica que comprende agua, un primer solvente orgánico, una primera base y un catalizador de metal de transicion a fin de producir Compuesto (4); iii) la oxidacion de compuesto 4 para producir Compuesto (5); iv) el agregado de un grupo amina a la posicion 6 de la porcion piridilo a fin de producir Compuesto (6); v) la reaccion de compuesto 6 con compuesto (7); en un segundo solvente orgánico, en presencia de una segunda base, a fin de producir compuesto (8); vi) la desesterificacion de compuesto 8 en un mezcla bifásica que comprende agua, un tercer solvente orgánico y un primer ácido, a fin de producir compuesto (9); vii) la suspension o disolucion de compuesto 9 en un solvente apropiado durante una cantidad eficaz de tiempo para producir Compuesto 1. Reivindicacion 26: Un compuesto de la formula (10); donde: R es H, alifático C1-6, arilo, aralquilo, heteroarilo, cicloalquilo, o heterocicloalquilo; R1 y R2 se seleccionan de manera independiente de -RgJ, -ORJ, -N(RJ)2, -NO2, halogeno, -CN, -haloalquiloC1-4, -haloalcoxiC1-4, -C(O)N(RJ)2, -NRJC(O)RJ, -SORJ, -SO2RJ, -SO2N(RJ)2, -NRJSO2RJ, -CORJ, -CO2RJ, -NRJSO2N(RJ)2, -COCORJ; RJ es hidrogeno o alifático C1-6; o es un numero entero de 0 a 3 inclusive; y p es un numero entero de 0 a 5 inclusive.
ARP100101869 2009-05-29 2010-05-28 Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos AR076897A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12/474,590 US20100036130A1 (en) 2007-12-07 2009-05-29 Processes for producing cycloalkylcarboxamido-pyridine benzoic acids

Publications (1)

Publication Number Publication Date
AR076897A1 true AR076897A1 (es) 2011-07-13

Family

ID=43223322

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101869 AR076897A1 (es) 2009-05-29 2010-05-28 Procesos para la produccion de acidos cicloalquilcarboxamido-piridina benzoicos

Country Status (4)

Country Link
US (4) US20100036130A1 (es)
AR (1) AR076897A1 (es)
TW (1) TWI589568B (es)
WO (1) WO2010138484A2 (es)

Families Citing this family (50)

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RU2006111093A (ru) 2003-09-06 2007-10-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Модуляторы атр-связывающих кассетных транспортеров
ZA200604578B (en) * 2003-11-14 2008-05-28 Vertex Pharma Thiazoles and oxazoles.useful as modulators of ATP Binding cassette transporters
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
CN104788328B (zh) 2004-06-24 2017-09-12 沃泰克斯药物股份有限公司 Atp‑结合弹夹转运蛋白的调控剂
JP5143738B2 (ja) 2005-08-11 2013-02-13 バーテックス ファーマシューティカルズ インコーポレイテッド 嚢胞性線維症膜コンダクタンス制御因子の調節物質
DK2774925T3 (en) * 2005-11-08 2017-02-27 Vertex Pharma Heterocyclic modulators of ATP binding cassette transporters
WO2007079139A2 (en) 2005-12-28 2007-07-12 Vertex Pharmaceuticals, Inc. Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
ES2398319T3 (es) * 2005-12-28 2013-03-15 Vertex Pharmaceuticals Incorporated Derivados de 1-(benzo[D][1,3]dioxol-5-il)-N-(fenil)ciclopropano-carboxamida y compuestos relacionados como moduladores de transportadores de casetes de unión a ATP para el tratamiento de la fibrosis quística
US7671221B2 (en) * 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
EP2007756B1 (en) 2006-04-07 2015-08-26 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US7645789B2 (en) * 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
AU2008251504B2 (en) 2007-05-09 2013-07-18 Vertex Pharmaceuticals Incorporated Modulators of CFTR
AU2008302598B2 (en) 2007-08-24 2014-07-17 Vertex Pharmaceuticals Incorporated Isothiazolopyridinones useful for the treatment of (inter alia) Cystic Fibrosis
DK2217572T3 (da) 2007-11-16 2014-02-03 Vertex Pharma Isoquinoliner som modulatorer af ATP-bindingskassettetransportører
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
EP2639222B1 (en) * 2007-12-07 2016-08-31 Vertex Pharmaceuticals Incorporated Process for producing cycloalkylcarboxiamido-pyridine benzoic acids
CN101998854A (zh) * 2007-12-07 2011-03-30 沃泰克斯药物股份有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的制剂
LT2225230T (lt) 2007-12-07 2017-01-25 Vertex Pharmaceuticals Incorporated 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il) benzoinės rūgšties kietos formos
CN102245573B (zh) 2008-02-28 2013-11-20 沃泰克斯药物股份有限公司 作为cftr调节剂的杂芳基衍生物
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US12458635B2 (en) 2008-08-13 2025-11-04 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
US20100074949A1 (en) 2008-08-13 2010-03-25 William Rowe Pharmaceutical composition and administration thereof
CN102164587A (zh) * 2008-09-29 2011-08-24 沃泰克斯药物股份有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的剂量单元
DK2349263T3 (da) * 2008-10-23 2014-07-21 Vertex Pharma Modulatorer af transmembranledningsevneregulatoren for cystisk fibrose
SG10201504084QA (en) 2009-03-20 2015-06-29 Vertex Pharma Process for making modulators of cystic fibrosis transmembrane conductance regulator
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
LT3150198T (lt) 2010-04-07 2021-12-10 Vertex Pharmaceuticals Incorporated 3-(6-(1-(2,2-difluorbenzo[d][1,3]dioksol-5-il) ciklopropankarboksamido)-3-metilpiridin-2-il)benzoinės rūgšties farmacinė kompozicija ir jos įvedimas
CN102933206A (zh) 2010-04-07 2013-02-13 弗特克斯药品有限公司 3-(6-(1-(2，2-二氟苯并[d][1，3]二氧杂环戊烯-5-基)环丙烷甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的固体形式
EP3381899B1 (en) 2010-04-22 2021-01-06 Vertex Pharmaceuticals Incorporated Intermediate compound for process of producing cycloalkylcarboxamido-indole compounds
US8563593B2 (en) 2010-06-08 2013-10-22 Vertex Pharmaceuticals Incorporated Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
IN2014KN00885A (es) 2011-11-08 2015-10-02 Vertex Pharma
JP2015504920A (ja) 2012-01-25 2015-02-16 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の製剤
CN109966264A (zh) 2012-02-27 2019-07-05 沃泰克斯药物股份有限公司 药物组合物及其施用
US8674108B2 (en) 2012-04-20 2014-03-18 Vertex Pharmaceuticals Incorporated Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
AU2013290444B2 (en) 2012-07-16 2018-04-26 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof
KR102280372B1 (ko) 2013-11-12 2021-07-22 버텍스 파마슈티칼스 인코포레이티드 Cftr 매개된 질환 치료용 약제학적 조성물의 제조 방법
JP6543268B2 (ja) 2014-04-15 2019-07-10 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ 嚢胞性線維症膜コンダクタンス調節因子が媒介する疾患を処置するための医薬組成物
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DK2217572T3 (da) 2007-11-16 2014-02-03 Vertex Pharma Isoquinoliner som modulatorer af ATP-bindingskassettetransportører
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CN101998854A (zh) * 2007-12-07 2011-03-30 沃泰克斯药物股份有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的制剂
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US8802700B2 (en) 2010-12-10 2014-08-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
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IN2014KN00885A (es) 2011-11-08 2015-10-02 Vertex Pharma
JP2015504920A (ja) 2012-01-25 2015-02-16 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ３−（６−（１−（２，２−ジフルオロベンゾ［ｄ］［１，３］ジオキソール−５−イル）シクロプロパンカルボキサミド）−３−メチルピリジン−２−イル）安息香酸の製剤
CN109966264A (zh) 2012-02-27 2019-07-05 沃泰克斯药物股份有限公司 药物组合物及其施用
US8674108B2 (en) 2012-04-20 2014-03-18 Vertex Pharmaceuticals Incorporated Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
AU2013290444B2 (en) 2012-07-16 2018-04-26 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof
CN104869982A (zh) 2012-11-02 2015-08-26 沃泰克斯药物股份有限公司 用于治疗cftr介导的疾病的药物组合物
US20140221424A1 (en) 2013-01-30 2014-08-07 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for use in the treatment of cystic fibrosis

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US20100036130A1 (en) 2010-02-11
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US20130274477A1 (en) 2013-10-17

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