AR053872A1 - Metodos para sintetizar 3- cianoquinolinas sustituidas y sus intermediarios - Google Patents
Metodos para sintetizar 3- cianoquinolinas sustituidas y sus intermediariosInfo
- Publication number
- AR053872A1 AR053872A1 ARP060102010A ARP060102010A AR053872A1 AR 053872 A1 AR053872 A1 AR 053872A1 AR P060102010 A ARP060102010 A AR P060102010A AR P060102010 A ARP060102010 A AR P060102010A AR 053872 A1 AR053872 A1 AR 053872A1
- Authority
- AR
- Argentina
- Prior art keywords
- phenyl
- alkyl
- alkylamino
- substituted
- hydroxy
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
- C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
Abstract
Los métodos son adecuados para la produccion a gran escala, evitar el uso de separaciones cromatográficas, y aportar un producto estable de pureza elevada, en forma más eficiente que en la técnica anterior. Reivindicacion 1: Un método para reparar 3-cianoquinolinas sustituidas que comprende el paso de hacer reaccionar (i) un compuesto de formula H-Z-(CH2)n-X, y (ii) una 3-cianoquinolina intermediaria que tiene la formula (1) en presencia de una cantidad catalítica eficaz de un catalizador ácido para producir un compuesto de formula (2) en donde X es un sistema de anillo arilo bicíclico o heteroarilo bicíclico de 8 a 12 átomos donde el anillo heteroarilo bicíclico contiene 1 a 4 heteroátomos seleccionados de N, O y S siempre que el anillo heteroarilo bicíclico no contenga enlaces O-O, S-S, o S-O y donde el anillo arilo bicíclico o heteroarilo bicíclico puede estar opcionalmente mono-, di-, tri o tetra-sustituido con un sustituyente seleccionado del grupo integrado por halogeno, oxo, tio, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, azido, hidroxialquilo C1-6, halometilo, alcoximetilo C2-7, alcanoiloximetilo C2-7, alcoxi C1-6, alquiltio C1-6, hidroxi, trifluormetilo, ciano, nitro, carboxi, carboalcoxi C2-7, carboalquilo C2-7, fenoxi, fenilo, tiofenoxi, benzoilo, bencilo, amino, alquilamino C1-6, dialquilamino C2-12, fenilamino, bencilamino, alcanoilamino C1-6, alquenoilamino C3-8, alquinoilamino C3-8, carboxialquilo C2-7, carboalcoxialquilo C3- 8,aminoalquilo C1-5, N-alquilaminoalquilo C2-9, N,N-dialquilaminoalquilo C3-10, N-alquilaminoalcoxi C2-9, N,N-dialquilaminoalcoxi C3-10, mercapto, y bencilamino; o X es cicloalquilo C3-7, el cual puede estar opcionalmente sustituido con uno o más grupos alquilo C1-6; o X es un anillo piridinilo, pirimidinilo, o fenilo, donde el anillo piridinilo, pirimidinilo o fenilo puede estar opcionalmente mono-, di- o tri sustituido con un sustituyentes seleccionado de grupo integrado por halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, azido, hidroxialquilo C1-6, halometilo, alcoximetilo C2-7, alcanoiloximetilo C2-7, alcoxi C1-6, alquiltio C1-6, hidroxi, trifluorometilo, ciano, nitro, carboxi, carboalcoxi C2-7, carboalquilo C2-7, fenoxi, fenilo, tiofenoxi, benzoilo, bencilo, amino, alquilamino C1-6, dialquilamino C2-12, fenilamino, bencilamino, alcanoilamino C1-6, alquenoilamino C3-8, alquinoilamino C3-8, y benzoilamino; o X es un radical que tiene la formula -A-T-L, donde A es un anillo piridinilo, pirimidinilo, o fenilo; donde el anillo piridinilo, pirimidinilo, o fenilo puede estar opcionalmente mono o di-sustituido con un sustituyente seleccionado del grupo integrado por halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, azido, hidroxialquilo C1-6, halometilo, alcoximetilo C2-7, alcanoiloximetilo C2-7, alcoxi C1-6, alquiltio C1-6, hidroxi, trifluormetilo, ciano, nitro, carboxi, carboalcoxi C2-7, carboalquilo C2-7, fenoxi, fenilo, tiofenoxi, benzoilo, bencilo, amino, alquilamino C1-6, dialquilamino C2-12, fenilamino, bencilamino, alcanoilamino C1-6, alquenoilamino C3-8, alquinoilamino C3-8, carboxialquilo C2-7, carboalcoxialquilo C3-8, aminoalquilo C1-5, N-alquilaminoalquilo C2-9, N,N- dialquilaminoalquilo C3-10, N-alquilaminoalcoxi C2-9, N,N-dialquilaminoalcoxi C3-10, mercapto, y benzoilamino; T está unido a un C de A y es: -NH(CH2)m-, -O(CH2)m-, -S(CH2)m-, -NR(CH2)m-, -(CH2)m-, -(CH2)mNH-, -(CH2)mO-, -(CH2)mS-, o -(CH2)mNR-; L es un anillo fenilo no sustituido o un anillo fenilo mono-, di o tri sustituido con un sustituyente seleccionado del grupo integrado por halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, azido, hidroxialquilo C1-6, halometilo, alcoximetilo C2- 7, alcanoiloximetilo C2-7, alcoxi C1-6, alquiltio C1-6, hidroxi, trifluormetilo, ciano, nitro, carboxi, carboalcoxi C2-7, carboalquilo C2-7, fenoxi, fenilo, tiofenoxi, benzoilo, bencilo, amino, alquilamino C1-6, dialquilamino C2-12, fenilamino, bencilamino, alcanoilamino C1-6, alquenoilamino C3-8, alquinoilamino C3-8, carboxialquilo C2-7, carboalcoxialquilo C3-8, aminoalquilo C1-5, N-alquilaminoalquilo C2-9, N,N-dialquilaminoalquilo C3-10, N-alquilaminoalcoxi C2-9, N,N-dialquilaminoalcoxi C3-10, mercapto, y benzoilamino; o L es un anillo heteroarilo de 5 o 6 miembros donde el anillo heteroarilo contiene 1 a 3 heteroátomos seleccionados de N, O y S, siempre que el anillo heteroarilo no contenga enlaces O-O, SS, o S-O, y donde el anillo heteroarilo está opcionalmente mono-, o di-sustituido con un sustituyente seleccionado del grupo integrado por halogeno, oxo, tio, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, azido, hidroxialquilo C1-6, halometilo, alcoximetilo C2-7, alcanoiloximetilo C2-7, alcoxi C1-6, alquiltio C1-6, hidroxi, trifluormetilo, ciano, nitro, carboxi, carboalcoxi C2-7, carboalquilo C2-7, fenoxi, fenilo, tiofenoxi, benzoilo, bencilo, amino, alquilamino C1-6, dialquilamino C2-12, fenilamino, bencilamino, alcanoilamino C1-6, alquenoilamino C3-8, alquinoilamino C3-8, carboxialquilo C2-7, carboalcoxialquilo C3-8, aminoalquilo C1-5, N-alquilaminoalquilo C2-9, N,N-dialquilaminoalquilo C3-10, N-alquilaminoalcoxi C2-9, N,N-dialquilaminoalcoxi C3-10, mercapto, y benzoilamino; LV es un grupo saliente; Z es -NH-, -O-, -S-, o -NR-; R es alquilo C1-6; G1, G2, R1 y R4 son cada uno, independientemente, H, halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alqueniloxi C2-6, alquiniloxi C2- 6, hidroximetilo, halometilo, alcanoiloxi C1-6, alquenoiloxi C3-8, alquinoiloxi C3-8, alcanoiloximetilo C2-7, alquenoiloximetilo C4-9, alquinoiloximetilo C4-9, alcoximetilo C2-7, alcoxi C1-6, alquiltio C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1- 6, alquilsulfonamido C1-6, alquenilsulfonamido C2-6, alquinilsulfonamido C2-6, hidroxi, trifluormetilo, trifluorometoxi, ciano, nitro, carboxi, carboalcoxi C2-7, carboalquilo C2-7, fenoxi, fenilo, tiofenoxi, bencilo, amino, hidroxiamino, alcoxiamino C1-4, alquilamino C1-6, dialquilamino C2-12, N-alquilcarbamoílo, N,N-dialquilcarbamoílo, N-alquil-alquenilamino C4-12, N,N-dialquenilamino C6-12, fenilamino, bencilamino, R7-(C(R6)2)p-N((C(R6)2)p)((C(R6)2)pN-(C(R6)2)k-Y-, R9R8-C(H)-M-(C(R6)2)k-Y- R7- (C(R6)2)g-Y-, R7-(C(R6)2)p-M-(C(R6)2)k-Y-, o Het-(C(R6)2)q-W-(C(R6)2-Y-; u opcionalmente G1 y/o G2 se seleccionan independientemente del grupo amino protegido y R2-NH-; Y es un radical divalente seleccionado del grupo integrado por -(CH2)a-, -O-, y - N(R6)-; R7 es -NR6R6, -OR6, -J, -N(R6)3+, o -NR6(OR6); M es >NR6, -O-, >N-(C(R6)2)pNR6R6, o >N-(C(R6)2)p-OR6; W es >NR6, -O- o es un enlace; Het se selecciona del grupo integrado por morfolina, tiomorfolina, tiomorfolina S-oxido, tiomorfolina S,S- dioxido, piperidina, pirrolidina, aziridina, piridina, imidazol, 1,2,3-triazol, 1,2,4-triazol, tiazol, tiazolidina, tetrazol, piperazina, furano, tiofeno, tetrahidrotiofeno, tetrahidrofurano, dioxano, 1,3-dioxolano, tetrahidropirano, y como se muestra en el resto de formula (3) donde Het está opcionalmente mono o di-sustituido sobre C o N con R6, opcionalmente mono o di-sustituida sobre C con hidroxi, -N(R6)2, u -OR6, opcionalmente mono o di-sustituido sobre C con los radicales monovalentes -(C(R6)2)sOR6 o -(C(R6)2)sN(R6)2, y opcionalmente mono o di-sustituido sobre un carbono saturado con radicales divalente -O- o -O(C(R6)2)sO-; R6 es H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C1-6, carboalquilo C2-7, carboxialquilo C2-7, fenilo, o fenilo opcionalmente sustituido con uno o más halogeno, alcoxi C1-6, trifluorometilo, amino, alquilamino C1-3, dialquilamino C2-6, nitro, ciano, azido, halometilo, alcoximetilo C2-7, alcanoiloximetilo C2-7, alquiltio C1-6, hidroxi, carboxilo, carboalcoxi C2-7, fenoxi, fenilo, tiofenoxi, benzoílo, bencilo, fenilamino, bencilamino, alcanoilamino C1-6, o alquilo C1-6, siempre que el resto alquenilo o alquinilo esté unido a un átomo de N u O a través de un átomo de C saturado; R2 se selecciona del grupo integrado por las formulas (4); R3 es independientemente H, alquilo C1-6, aminoalquilo C1-6, cicloaminoalquilo C4-12, carboxi, carboalcoxi C1-6, fenilo, carboalquilo C2-7, R7-((R6)2C)p-N-(C(R6)2)p(C(R6)2)p-N- (C(R6)2)-; R7-(C(R6)2)s-; R7(C(R6)2)p-M-(C(R7)2)r-, R8R9-CH-M-(C(R6)2)r-, o Het-(C(R6)2)q-W-(C(R6)2)r-; R5 es independientemente H, alquilo C1-6, carboxi, carboalcoxi C1-6, fenilo, carboalquilo C2-7, R7-((R6)2C)p-N-(C(R6)2)p(C(R6)2)p-N-(CH2(R6)2)r-; R7-(C(R6)2)s-; R7(C(R6)2)p-M-(C(R6)2)r-, R8R9-CH-M-(C(R6)2)r-, o Het-(C(R6)2)q-W-(C(R6)2)r-, R8 y R9 son cada uno, independientemente, -(C(R6)2)rNR6R6, o -(C(R6)2)rOR6; J es independientemente H, Cl, F o Br; Q es alquilo C1-6 o H; a= 0 o 1; g= 1-6; k= 0-4; m es 0-3; n es 0-1; p= 2-4; q= 0-4; r= 1-4; s= 1-6; u= 0-4 y v=0-4, donde la suma de u+v es 2-4.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US68439105P | 2005-05-25 | 2005-05-25 |
Publications (1)
Publication Number | Publication Date |
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AR053872A1 true AR053872A1 (es) | 2007-05-23 |
Family
ID=37037465
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP060102010A AR053872A1 (es) | 2005-05-25 | 2006-05-18 | Metodos para sintetizar 3- cianoquinolinas sustituidas y sus intermediarios |
Country Status (19)
Country | Link |
---|---|
US (1) | US20060270668A1 (es) |
EP (1) | EP1883631A1 (es) |
JP (1) | JP2008545688A (es) |
KR (1) | KR20080016671A (es) |
CN (1) | CN101203494A (es) |
AR (1) | AR053872A1 (es) |
AU (1) | AU2006249600A1 (es) |
BR (1) | BRPI0610147A2 (es) |
CA (1) | CA2609186A1 (es) |
CR (1) | CR9544A (es) |
GT (1) | GT200600213A (es) |
IL (1) | IL187532A0 (es) |
NO (1) | NO20076067L (es) |
PA (1) | PA8676201A1 (es) |
PE (1) | PE20061417A1 (es) |
RU (1) | RU2007143161A (es) |
TW (1) | TW200716557A (es) |
WO (1) | WO2006127207A1 (es) |
ZA (1) | ZA200710148B (es) |
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UA85698C2 (ru) * | 2004-01-16 | 2009-02-25 | Уайет | Хинолиновые промежуточные соединения для синтеза ингибиторов рецепторной тирозинкиназы и способ их получения |
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- 2006-04-28 EP EP06769913A patent/EP1883631A1/en not_active Withdrawn
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- 2006-04-28 BR BRPI0610147-0A patent/BRPI0610147A2/pt not_active IP Right Cessation
- 2006-04-28 JP JP2008513498A patent/JP2008545688A/ja not_active Withdrawn
- 2006-04-28 AU AU2006249600A patent/AU2006249600A1/en not_active Abandoned
- 2006-04-28 CA CA002609186A patent/CA2609186A1/en not_active Abandoned
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- 2006-04-28 KR KR1020077030160A patent/KR20080016671A/ko not_active Application Discontinuation
- 2006-04-28 RU RU2007143161/04A patent/RU2007143161A/ru unknown
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TW200716557A (en) | 2007-05-01 |
JP2008545688A (ja) | 2008-12-18 |
IL187532A0 (en) | 2008-03-20 |
WO2006127207A1 (en) | 2006-11-30 |
PA8676201A1 (es) | 2009-03-31 |
EP1883631A1 (en) | 2008-02-06 |
NO20076067L (no) | 2007-12-21 |
KR20080016671A (ko) | 2008-02-21 |
CN101203494A (zh) | 2008-06-18 |
CA2609186A1 (en) | 2006-11-30 |
ZA200710148B (en) | 2008-09-25 |
US20060270668A1 (en) | 2006-11-30 |
RU2007143161A (ru) | 2009-07-10 |
GT200600213A (es) | 2007-01-12 |
CR9544A (es) | 2008-03-07 |
AU2006249600A1 (en) | 2006-11-30 |
PE20061417A1 (es) | 2007-01-20 |
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