MX2016000386A - Proceso para la preparacion de un intermediario de pirimidina. - Google Patents

Proceso para la preparacion de un intermediario de pirimidina.

Info

Publication number
MX2016000386A
MX2016000386A MX2016000386A MX2016000386A MX2016000386A MX 2016000386 A MX2016000386 A MX 2016000386A MX 2016000386 A MX2016000386 A MX 2016000386A MX 2016000386 A MX2016000386 A MX 2016000386A MX 2016000386 A MX2016000386 A MX 2016000386A
Authority
MX
Mexico
Prior art keywords
preparing
macitentan
bromophenyl
pyrimidinyl
oxy
Prior art date
Application number
MX2016000386A
Other languages
English (en)
Other versions
MX360768B (es
Inventor
Stefan Abele
Jacques-Alexis Funel
Ivan Schindelholz
Original Assignee
Actelion Pharmaceuticals Ltd
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 Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of MX2016000386A publication Critical patent/MX2016000386A/es
Publication of MX360768B publication Critical patent/MX360768B/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/30Halogen atoms or nitro radicals

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Detergent Compositions (AREA)
  • Magnetic Heads (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Manufacturing Cores, Coils, And Magnets (AREA)
  • Extraction Or Liquid Replacement (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

La invención se refiere a un proceso para la preparación de un intermediario de pirimidina es decir, el compuesto de la fórmula I-2 o una de sus sales. Dicho compuesto de la fórmula 1-2 o su sal puede ser usado para la preparación de macitentan. Macitentan (denominaciones químicas: N-[5-(4-bromofenil)-6-[2-[(5-bromo-2-pir imidinil)oxi]etoxi]-4-pirimidinil]-N'-propilsulfamida o N-[5-(4-bromofenil)-6-{2-[(5-bromopirimidin-2-il)oxi]etoxi}pirimi din-4-il]-N'-propilsulfúrico diamida) es un antagonista del receptor de endotelina que ha sido notablemente aprobado por la Administración de Drogas y Medicamentos de los Estados Unidos y la Comisión Europea para el tratamiento de la hipertensión arterial pulmonar. Se divulgó por primera vez en la Solicitud Internacional WO 02/053557. La última etapa de una de las posibles vías de preparación que se describen en la Solicitud Internacional WO 02/053557, denominada "Posibilidad A" y "Posibilidad B", puede resumirse como se muestra en el Esquema A1 a continuación.
MX2016000386A 2013-07-12 2014-07-11 Proceso para la preparacion de un intermediario de pirimidina. MX360768B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13176374 2013-07-12
PCT/EP2014/064904 WO2015004265A1 (en) 2013-07-12 2014-07-11 Process for preparing a pyrimidine intermediate

Publications (2)

Publication Number Publication Date
MX2016000386A true MX2016000386A (es) 2016-04-29
MX360768B MX360768B (es) 2018-11-15

Family

ID=48790244

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016000386A MX360768B (es) 2013-07-12 2014-07-11 Proceso para la preparacion de un intermediario de pirimidina.

Country Status (17)

Country Link
US (1) US9556125B2 (es)
EP (1) EP3019479B1 (es)
JP (1) JP6375374B2 (es)
KR (1) KR102305298B1 (es)
CN (1) CN105636940B (es)
AR (1) AR096865A1 (es)
CA (1) CA2915736C (es)
DK (1) DK3019479T3 (es)
ES (1) ES2636937T3 (es)
HR (1) HRP20171166T1 (es)
HU (1) HUE034071T2 (es)
IL (1) IL243477B (es)
MX (1) MX360768B (es)
PL (1) PL3019479T3 (es)
PT (1) PT3019479T (es)
TW (1) TWI643848B (es)
WO (1) WO2015004265A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA201605808B (en) 2015-08-26 2017-08-30 Cipla Ltd Process for preparing an endothelin receptor antagonist
CN105461638A (zh) * 2015-12-10 2016-04-06 合肥久诺医药科技有限公司 一种马西替坦晶型及其制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0116237B8 (pt) 2000-12-18 2021-05-25 Actelion Pharmaceuticals Ltd "composto de sulfamida, composição farmacêutica contendo o mesmo e seu uso como medicamento antagonista de receptor de endotelina".
CN103724281A (zh) * 2013-12-03 2014-04-16 镇江圣安医药有限公司 N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]-n′-丙基磺酰胺的新型衍生物及其应用
CN103819411A (zh) * 2014-03-14 2014-05-28 成都克莱蒙医药科技有限公司 一种马西替坦中间体新的制备方法

Also Published As

Publication number Publication date
EP3019479B1 (en) 2017-05-10
JP6375374B2 (ja) 2018-08-15
KR20160030972A (ko) 2016-03-21
EP3019479A1 (en) 2016-05-18
PT3019479T (pt) 2017-08-11
IL243477B (en) 2018-06-28
HRP20171166T1 (hr) 2017-10-06
WO2015004265A1 (en) 2015-01-15
CN105636940A (zh) 2016-06-01
CN105636940B (zh) 2018-02-27
MX360768B (es) 2018-11-15
US9556125B2 (en) 2017-01-31
PL3019479T3 (pl) 2017-10-31
TW201536759A (zh) 2015-10-01
HUE034071T2 (en) 2018-01-29
ES2636937T3 (es) 2017-10-10
US20160145215A1 (en) 2016-05-26
CA2915736A1 (en) 2015-01-15
CA2915736C (en) 2021-07-27
DK3019479T3 (en) 2017-07-17
AR096865A1 (es) 2016-02-03
TWI643848B (zh) 2018-12-11
JP2016525094A (ja) 2016-08-22
KR102305298B1 (ko) 2021-09-27

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