CO5080807A1 - Produccion de alcoholes a partir de sulfato ciclico - Google Patents

Produccion de alcoholes a partir de sulfato ciclico

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Publication number
CO5080807A1
CO5080807A1 CO99041717D CO99041717D CO5080807A1 CO 5080807 A1 CO5080807 A1 CO 5080807A1 CO 99041717 D CO99041717 D CO 99041717D CO 99041717 D CO99041717 D CO 99041717D CO 5080807 A1 CO5080807 A1 CO 5080807A1
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alkyl
heterocycle
quaternary
heteroaryl
alkynyl
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CO99041717D
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English (en)
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F Lee Len
C Banerjee Shyamal
Huang Horng-Chih
J Li Jinglin
Raymond E Miller
David B Reitz
Samuel J Tremont
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Searle & Co
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Publication of CO5080807A1 publication Critical patent/CO5080807A1/es

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    • A—HUMAN NECESSITIES
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D337/02—Seven-membered rings
    • C07D337/06—Seven-membered rings condensed with carbocyclic rings or ring systems
    • C07D337/08—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with one six-membered ring
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    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07F9/655381—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a seven-(or more) membered ring
    • C07F9/65539—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a seven-(or more) membered ring condensed with carbocyclic rings or carbocyclic ring systems
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    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
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    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds

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Abstract

Un proceso para la preparación de un compuesto de fórmula: <EMI FILE="99041717_1" ID="1" IMF=JPEG >que comprende tratar un tiofenol con un agente extrayente; acoplar el tiofenol y un sulfato cíclico para formar un intermedio que comprende un grupo sulfato; y remover el grupo sulfato del intermedio para formar el compuesto de la fórmula XLI; en donde q es un entero de 1 a 4; R1 y R2 son independientemente seleccionados a partir del grupo consistente de H, alquilo, alquenilo, alquinilo, haloalquilo, alquilarilo, arilalquilo, alcoxi, alcoxialquilo, dialquilamino, alquiltio, (polialquilo)arilo y cicloalquilo, en donde alquilo, alquenilo, alquinilo, haloalquilo, alquilarilo, arilalquilo, alcoxi, alcoxialquilo, dialquilamino, alquiltio, (polialquilo)arilo, y cicloalquilo opcionalmente son sustituidos con uno o más sustituyentes seleccionados del grupo consistente de OR9 , NR9R10, N+R9R10RwA-, SR9, S+R9R10A-, P+R9R10R11A-, S(O)R9, S02R9, S03R9, C02R9, CN, halógeno, oxo, y CONR9 R10,en donde alquilo, alquenilo, alquinilo, alquilarilo, alcoxi, alcoxialquilo, (polialquilo)arilo y cicloalquilo, opcionalmente tienen uno o más carbonos reemplazados por O, NR9, N+R9 R10A-, S, SO, S02, S+R9 A-, P+R9 R10A-, o fenileno,en donde R9, R10, y Rw son independiente seleccionados del grupo que consiste de H, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, acilo, heterociclo, amonioalquilo, arilalquilo, carboxialquilo, carboxiheteroarilo, carboxiheterociclo, carboalcoxialquilo, carboxialquilamino, heteroarilalquilo, heterociclilalquilo, y alquilamonioalquilo; oR1 y R2 tomados juntos con el carbono al cual ellos están adheridos forman un cicloalquilo C3-C10;R3 es hidroxi;R4 es hidrógeno;R5 y R6 son independientemente seleccionados del grupo consistente de H, alquilo, alquenilo, alquinilo, arilo, cicIoalquilo, heterociclo, heterociclo cuaternario, OR30, SR9 , S(0)R9 , S02R9, y S03R9, R6 es seleccionado del grupo consistente de H, alquilo, alquenilo, alquinilo, arilo, cicloalquilo, heterociclo, heterociclo cuatemario, OR30, SR9, S(0)R9, S02R9, y S03R9,- 2 - en donde alquilo, alquenilo, alquinilo, arilo, cicloalquilo, heterociclo, heterociclo cuaternario, y heteroarilo cuatemario pueden ser sustituidos con uno o más grupos sustituyentes independientemente seleccionados del grupo que consiste de alquilo, alquenilo, alquinilo, polialquilo, poliéter, arilo, haloalquilo, cicloalquilo, heterociclo, arilalquilo, heterociclo cuaternario, heteroarilo cuaternario, halógeno, oxo, OR13, NR13R14, SR13, S(0)R13, S02R13, S03R13, NR13OR14, NR13NR14R15, NO2, C02R13, CN, OM, S020M, S02NR13R14, C(0)NR13R14, C(O)OM, COR13, NR13C(0)R14, NR13C(0)NR14R15, NR13C02R14, OC(0)R13, OC(0)NR13R14, NR13SOR14, NR13S02R14, NR13S0NR14R15, NR13S02NR14R15, P(0)R13R14, P+R13R14R15A-, P(OR13)OR14, S+R13R14A-, y N+R9R11R12A-, en donde A- es un anión farmacéuticamente aceptable y M es un catión farmacéuticamente aceptable, dichos alquilo, alquenilo, alquinilo, polialquilo, poliéter, arilo, haloalquilo, cicloalquilo, y heterociclo pueden ser adicionalmente sustituidos con uno o más grupos sustituyentes seleccionados a partir del grupo que consiste de OR7, NR7R8, SR7, S(O)R7, S02R7, SO3R7, C02R7, CN, oxo, CONR7R8, N+R7R8R9A-, alquilo, alquenilo, alquinilo, arilo, cicloalquilo, heterociclo, arilalquilo, heterociclo cuaternario, heteroarilo cuaternario, P(0)R7R8, P+R7R8R9A-, y P(0)(OR7)OR8, y en donde dicho alquilo, alquenilo, alquinilo, polialquilo, poliéter, arilo, haloalquilo, cicloalquilo y heterociclo pueden opcionalmente tener uno o más carbonos reemplazados por O, NR7, N+R7R8A-, S, SO, S02, S+R7A-, PR7, P(0)R7, P+R7R8A-, o fenileno, y R13, R14, y R15 son independiente seleccionados a partir del grupo que consiste de hidrógeno, alquilo, alquenilo, alquinilo, polialquilo, poliéter, arilo, arilalquilo, alquilarilalquilo, alquilheteroarilalquilo, alquilheterociclilalquilo, cicloalquilo, heterociclo, heteroarilo, heterociclo cuaternario, heteroarilo cuaternario, heterociclilalquilo, heteroarilalquilo, heterociclilalquilo cuaternario, heteroarilalquilo cuaternario, alquilamonioalquilo, y carboxialquilaminocarbonilalquilo,en donde alquilo, alquenilo, alquinilo, arilalquilo, heterociclo, y polialquilo opcionalmente tienen uno o más carbonos reemplazados por O, NR9 , N+R9R1OA-, S, SO, S02, S+R9A-, PR9, P+R9R10A-, P(0)R9, fenileno, carbohidrato, aminoácido, péptido, o polipéptido, y R13, R14 y R15 son opcionalmente sustituidos con uno más grupos seleccionados a partir del grupo que consiste de hidroxi, amino, sulfo, carboxi, alquilo, carboxialquilo, heterociclo, heteroarilo, sulfoalquilo, heterociclo cuaternario, heteroarilo cuaternario, heterociclilalquilo cuaternario, heteroarilalquilo cuaternario, guanidinilo, OR9, NR9R10, N+R9R11R12A-, SR9 , S(0)R9, S02R9, SO3R9, oxo, C02R9, CN, halógeno, CONR9R10, S020M, S02NR9 R10, PO(OR16)OR17, P+R9R10R11A-, S+R9R10A-, y C(O)OM, en donde R16 y R17 son independientemente seleccionados de los sustituyentes que constituyen R9 y M; o R13 y R14, junto con el átomo de nitrógeno junto al cual están unidos, forman un heterociclo mono- o policíclico que está opcionalmente sustituido con uno o más radicales seleccionados del grupo consistente de oxo, carboxi, y sales cuaternarias; o R14 y R15, juntos con el átomo de nitrógeno, al cual están enlazados, forman un anillo cíclico; y R30 es seleccionado del grupo consistente de alquilo, alquenilo, alquinilo, cicloalquilo, arilo, acilo, heterociclo, amonioalquilo, alquilamonioalquilo, arilalquilo, carboxialquilo, carboxiheteroarilo, carboxiheterociclo, carboalcoxialquilo, carboxialquilamino, heteroarilalquilo, heterociclilalquilo, y alquilamonioalquilo; y R7 y R8 son independientemente seleccionados del grupo consistente de hidrógeno y alquilo; y uno o más Rx son independiente seleccionados del grupo que consiste de H, alquilo, alquenilo, alquinilo, polialquilo, aciloxi, arilo, alrilalquilo, halógeno, haloalquilo, cicloalquilo, heterociclo, heteroarilo, poliéter, heterociclo cuaternario, heteroarilo cuaternario, OR13, NR13R14, SR13, S(0)R13, S(0)2R13, S03R13, S+R13R14A-, NR130R14, NR13NR14R15, NO2, C02R13, CN, OM, S020M, S02NR13R14, NR14C(0)R13, C(0)NR13R14, NR14C(0)R13, C(O)OM, COR13, OR18, S(0)nNR18, NR13R18, NR180R14, N+R9R11R12A-, P+R9R11R12A-, aminoácido, péptido, polipéptido y carbohidrato, en donde alquilo, alquenilo, alquinilo, cicloalquilo, arilo, polialquilo, heterociclo, aciloxi, arilalquilo, haloalquilo, poliéter, heterociclo cuaternario, y heteroarilo cuaternario pueden adicionalmente ser sustituidos con OR9 , NR9R10, N+R9R11R12A-, SR9, S(0)R9, S02R, SO3R9 , oxo, C02R9, CN, halógeno, CONR9R10, S02OM, S02NR9R10, PO(OR16)OR17, P+R9R11R12A-, S+R9R10A-, o C(O)OM, y en donde R18 es seleccionado del grupo que consiste de acilo, arilalcoxicarbonilo, arilalquilo, heterociclo, heteroarilo, y alquilo, en donde acilo, arilalcoxicarbonilo, arilalquilo, heterociclo, heteroarilo, alquilo, heterociclo cuaternario, y heteroarilo cuaternario opcionalmente están sustituidos con uno o más sustituyentes seleccionados a partir del grupo que consiste de OR9, NR9R10, N+R9R11R12A-, SR9, S(0)R9, S02R9, SO3R9, oxo, C02R9 , CN, halógeno, CONR9R10, SO3R9, S02OM, S02NR9R10, PO(OR16)OR17, y C(O)OM, - 3 -en donde en Rx, uno o más carbonos son opcionalmente reemplazados por O, NR13, N+R13R14A-, S, SO, S02, S+R13A-, PR13, P(0)R13, P+R13R14A-, fenileno, aminoácido, péptido, polipéptido, carbohidrato, poliéter, o polialquilo,en donde en dicho polialquilo, fenileno, aminoácido, péptido, polipéptido, y carbohidrato, uno o más carbonos son opcionalmente reemplazados por O, NR9, N+R9R1OA-, S, SO, SO2, S+R9A-, PR9 , P+R9R10A-, o P(0)R9 ; en donde el heterociclo cuaternario y el heteroarilo cuatemario son opcionalmente sustituidos con uno o más grupos seleccionados a partir del grupo que consiste de alquilo, alquenilo, alquinilo, polialquilo, poliéter, arilo, haloalquilo, cicloalquilo, heterociclo, arilalquilo, halógeno, oxo, OR13, NR13R14, SR13, S(0)R13, S02R13, SO3R13, NR13OR14, NR13NR14R15, NO2, C02R13, CN, OM, S02OM, S02NR13R14, C(0)NR13R14, C(O)OM, COR13, P(0)R13R14, P+R13R14R15A-, P(OR13)OR14, S+R13R14A-, y N+R9R11R12A-.
CO99041717D 1998-07-02 1999-07-02 Produccion de alcoholes a partir de sulfato ciclico CO5080807A1 (es)

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US09/109,551 US5994391A (en) 1994-09-13 1998-07-02 Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake

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