CL2012001140A1 - Proceso para la preparacion de derivados de 5-(2-aminopirimidin-4-il)-2-aril-1h-pirrol-3-carboxamidas; compuestos intermediarios considerados; y la preparacion de los mismos. - Google Patents

Proceso para la preparacion de derivados de 5-(2-aminopirimidin-4-il)-2-aril-1h-pirrol-3-carboxamidas; compuestos intermediarios considerados; y la preparacion de los mismos.

Info

Publication number
CL2012001140A1
CL2012001140A1 CL2012001140A CL2012001140A CL2012001140A1 CL 2012001140 A1 CL2012001140 A1 CL 2012001140A1 CL 2012001140 A CL2012001140 A CL 2012001140A CL 2012001140 A CL2012001140 A CL 2012001140A CL 2012001140 A1 CL2012001140 A1 CL 2012001140A1
Authority
CL
Chile
Prior art keywords
formula
preparation
resulting compound
aminopyrimidin
salt
Prior art date
Application number
CL2012001140A
Other languages
English (en)
Inventor
Mateo D'anello
Marco Re
Original Assignee
Nerviano Medical Sciences Srl
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 Nerviano Medical Sciences Srl filed Critical Nerviano Medical Sciences Srl
Publication of CL2012001140A1 publication Critical patent/CL2012001140A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

PROCESO PARA PREPARAR UNA 5-(2-AMINOPIRIMIDIN-4-IL)-2-ARIL-1H-PIRROL-3-CARBOXAMIDA DE LA FÓRMULA (I) DONDE R1 Y R2, QUE COMPRENDE A) ACOPLAR UN ACETAL DE FÓRMULA (II) Y FORMA UN ACETAL CICLICO, CON UN BETA-CETOÉSTER O UNA SAL DEL MISMO DE FÓRMULA (III); B) ACETILAR EL COMPUESTO RESULTANTE DE LA FÓRMULA (IV) CON UN HALURO DE ACETILO O ANHÍDRIDO ACÉTICO EN PRESENCIA DE UN ÁCIDO DE LEWIS; C) HACER REACCIONAR EL COMPUESTO RESULTANTE DE FORMULA (V) CON UN C,-C, DIALQUIL ACETAL DE N,N-DIMETIL- FORMAMIDA; D) HACER REACCIONAR LA ENAMINONA RESULTANTE DE FÓRMULA (VI) CON GUANIDINA O UNA SAL DE LA MISMA; E) HIDROLIZAR EL GRUPO ÉSTER CARBOXILICO DEL COMPUESTO RESULTANTE DE FÓRMULA (VII); F) CONDENSAR EL GRUPO ÁCIDO CARBOXÍLICO DEL COMPUESTO RESULTANTE DE FÓRMULA (VIII) CON UNA FORMA DE AMONIACO, PARA DAR LA CARBOXAMIDA DE FÓRMULA (I); Y, SI SE DESEA, CONVERTIRLA EN UNA SAL FARMACÉUTICAMENTE ACEPTABLE;<br /> COMPUESTOS INTERMEDIARIOS DE FÓRMULA (IV') Y (V); Y ENAMINONA INTERMEDIARIA DE FÓRMULA (VI).<br />  
CL2012001140A 2009-11-04 2012-04-30 Proceso para la preparacion de derivados de 5-(2-aminopirimidin-4-il)-2-aril-1h-pirrol-3-carboxamidas; compuestos intermediarios considerados; y la preparacion de los mismos. CL2012001140A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09175063 2009-11-04

Publications (1)

Publication Number Publication Date
CL2012001140A1 true CL2012001140A1 (es) 2012-08-31

Family

ID=43431011

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2012001140A CL2012001140A1 (es) 2009-11-04 2012-04-30 Proceso para la preparacion de derivados de 5-(2-aminopirimidin-4-il)-2-aril-1h-pirrol-3-carboxamidas; compuestos intermediarios considerados; y la preparacion de los mismos.

Country Status (15)

Country Link
US (1) US8592583B2 (es)
EP (1) EP2496570B1 (es)
JP (1) JP5715146B2 (es)
CN (1) CN102666527B (es)
AR (1) AR078883A1 (es)
AU (1) AU2010314204B2 (es)
BR (1) BR112012010445B1 (es)
CA (1) CA2779785C (es)
CL (1) CL2012001140A1 (es)
EA (1) EA021299B1 (es)
ES (1) ES2593630T3 (es)
HK (1) HK1175781A1 (es)
MX (1) MX339634B (es)
TW (1) TWI478914B (es)
WO (1) WO2011054714A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2621732C2 (ru) * 2011-04-19 2017-06-07 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные пиримидинилпирролы, активные в качестве ингибиторов киназы
CN107915720B (zh) * 2016-10-08 2020-09-11 常州市第四制药厂有限公司 沃诺拉赞的新制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH09295967A (ja) * 1996-05-02 1997-11-18 Sumitomo Metal Ind Ltd 新規ピロールアルカン酸誘導体
SE0202463D0 (sv) * 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
WO2005074643A2 (en) * 2004-01-30 2005-08-18 Smithkline Beecham Corporation Benzamide compounds useful as rock inhibitors
WO2007026920A2 (en) * 2005-09-02 2007-03-08 Astellas Pharma Inc. Amide derivatives as rock inhibitors
KR101616388B1 (ko) * 2006-03-27 2016-04-29 네르비아노 메디칼 사이언시스 에스.알.엘. 키나제 억제제로서의 피리딜- 및 피리미디닐-치환된 피롤-, 티오펜- 및 푸란-유도체
TWI426074B (zh) * 2008-04-30 2014-02-11 Nerviano Medical Sciences Srl ５－（２－胺基－嘧啶－４－基）－２－芳基－１ｈ－吡咯－３－羧醯胺之製造方法

Also Published As

Publication number Publication date
MX339634B (es) 2016-06-02
US8592583B2 (en) 2013-11-26
EA021299B1 (ru) 2015-05-29
EA201290276A1 (ru) 2012-12-28
CN102666527B (zh) 2014-10-01
WO2011054714A1 (en) 2011-05-12
US20120220771A1 (en) 2012-08-30
BR112012010445B1 (pt) 2021-09-21
CN102666527A (zh) 2012-09-12
AU2010314204B2 (en) 2015-03-26
AU2010314204A1 (en) 2012-06-21
CA2779785C (en) 2017-09-12
EP2496570A1 (en) 2012-09-12
ES2593630T3 (es) 2016-12-12
BR112012010445A2 (pt) 2015-09-29
JP5715146B2 (ja) 2015-05-07
EP2496570B1 (en) 2016-06-29
CA2779785A1 (en) 2011-05-12
JP2013510110A (ja) 2013-03-21
TWI478914B (zh) 2015-04-01
AR078883A1 (es) 2011-12-07
HK1175781A1 (en) 2013-07-12
MX2012004844A (es) 2012-06-12
TW201121954A (en) 2011-07-01

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