AR064312A1 - Procedimientos para la preparacion de 3-(4-(2,4-difluorobenciloxi)-3-bromo-6-metil-2-oxopiridin-1(2h)-il)-n,4-dimetilbenzamida - Google Patents

Procedimientos para la preparacion de 3-(4-(2,4-difluorobenciloxi)-3-bromo-6-metil-2-oxopiridin-1(2h)-il)-n,4-dimetilbenzamida

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AR064312A1
AR064312A1 ARP070105576A ARP070105576A AR064312A1 AR 064312 A1 AR064312 A1 AR 064312A1 AR P070105576 A ARP070105576 A AR P070105576A AR P070105576 A ARP070105576 A AR P070105576A AR 064312 A1 AR064312 A1 AR 064312A1
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compound
formula
contacting
alkyl
produce
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ARP070105576A
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English (en)
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G Klemm
R Vanderroest
B Chekal
M Mao
Embse R Vonder
R Geurnik
G Yalamanchili
R Valdyanathan
D Dukeshereer
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Pfizer Prod Inc
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Publication of AR064312A1 publication Critical patent/AR064312A1/es

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    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/64One oxygen atom attached in position 2 or 6
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
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Abstract

Procedimientos para la preparacion de compuestos de la formula 1 en la que R2, R3, R4, R5, XI, X2, X3, X4, X5, X6 son como se definen en la memoria descriptiva. Reivindicacion 1: Un procedimiento caracterizado porque es para la preparacion de un compuesto de la formula 1, que comprende las etapas: a) poner en contacto un compuesto de la formula 5, con un reactivo de halogenacion en presencia de al menos un disolvente para producir un compuesto de la formula 4, b) poner en contacto un compuesto de la formula 4 con una hidrolasa en presencia de una solucion tampon para producir un compuesto de la formula 10, c) poner en contacto un compuesto de la formula 10 con un reactivo activante en presencia de al menos un disolvente y después poner en contacto la mezcla resultante con una amina para producir un compuesto de la formula 9; y d) poner en contacto un compuesto de la formula 9 con un haluro de bencilo sustituido en presencia de una base y al menos un disolvente para producir un compuesto de la formula 1; en el X1, X2, X3, X4, X5 y X6 son independientemente H, halo, o un alquilo C1-6; R1 es un alquilo C 1-6 o arilo; R2 es H, halo, o un alquilo C1-6; R3 es halo, o un alquilo C1-6; y R4 es H o un alquilo C1-6; R5 es H, un alquilo C1-6 o arilo; o R4, R5, y el nitrogeno al que están unidos forman un anillo morfolinilo, tiomorfolinilo, piperidinilo, pirrolidinilo, o piperazinilo que está opcionalmente sustituido con 1 o 2 grupos que son independientemente alquilo C1-4, alcoxi C1-4, hidroxi,.hidroxi-alquiIo C1-4,dihidroxi-alquilo C1-4, o halogeno. Reivindicacion 20: Un procedimiento para la preparacion de un compuesto de la formula 1 caracterizado porque tiene la siguiente estructura: que comprende las etapas: a) poner en contacto un compuesto de la formula 5 con 1,3-dibromo-5,5-dimetilhidantoína en presencia de acetonitrilo para producir un compuesto de la formula 4; b) poner en contacto un compuesto de la formula 4 con proteasa de Bacillus sp. En presencia de una solucion tampon de fosfato de potasio para producir un compuesto de la formula 10; c) poner en contacto un compuesto de la formula 10 con 1,1'-carbonildiimidazol en presencia de dimetilformamida y después se pone en contacto la mezcla resultante con NH2CH3 en tetrahidrofurano para producir un compuesto de la formula 9; y d) poner en contacto un compuesto de la formula 9 con un compuesto que tiene la estructura (1) en presencia de carbonato de potasio y N- metilpirrolidinona.
ARP070105576A 2006-12-13 2007-12-12 Procedimientos para la preparacion de 3-(4-(2,4-difluorobenciloxi)-3-bromo-6-metil-2-oxopiridin-1(2h)-il)-n,4-dimetilbenzamida AR064312A1 (es)

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US86974806P 2006-12-13 2006-12-13

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AR064312A1 true AR064312A1 (es) 2009-03-25

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US (1) US7906536B2 (es)
EP (1) EP2102161B1 (es)
JP (1) JP2008231090A (es)
KR (1) KR20090090379A (es)
CN (1) CN101611006A (es)
AR (1) AR064312A1 (es)
AT (1) ATE556055T1 (es)
AU (1) AU2007331199A1 (es)
BR (1) BRPI0720757A2 (es)
CA (1) CA2672256C (es)
IL (1) IL199239A0 (es)
MX (1) MX2009006266A (es)
NZ (1) NZ577639A (es)
RU (1) RU2411236C1 (es)
TW (1) TW200837057A (es)
WO (1) WO2008072079A2 (es)
ZA (1) ZA200903981B (es)

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JP5679159B2 (ja) 2010-07-05 2015-03-04 信越化学工業株式会社 希土類金属抽出剤の合成方法、及び希土類金属の溶媒抽出用有機相
WO2014181213A1 (en) 2013-05-10 2014-11-13 Pfizer Inc. Crystalline form of (sa)-(-)-3-(3-bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1 (2h)-yl)-n,4-dimethylbenzamide
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
PL3976589T3 (pl) * 2019-10-18 2023-07-31 Fmc Corporation Sposoby wytwarzania kwasu 5-bromo-2-(3-chloropirydyn-2-ylo)-2H-pirazolo-3-karboksylowego

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JP3286645B2 (ja) * 1993-03-26 2002-05-27 メルシャン株式会社 光学活性1,4−ジヒドロピリジン誘導体およびその製造方法
EP1490064B1 (en) 2002-02-14 2009-11-18 Pharmacia Corporation Substituted pyridinones as modulators of p38 map kinase
NL1026826C2 (nl) * 2003-08-13 2007-01-04 Pharmacia Corp Gesubstitueerde pyridinonen.
CN101027404A (zh) * 2004-08-26 2007-08-29 辉瑞大药厂 对映选择性生物转化制备蛋白酪氨酸激酶抑制剂中间体
CA2640665A1 (en) * 2006-02-10 2007-08-16 Pfizer Products Inc. Pyridinone pyrazole urea and pyrimidinone pyrazole urea derivatives

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US7906536B2 (en) 2011-03-15
TW200837057A (en) 2008-09-16
CN101611006A (zh) 2009-12-23
RU2411236C1 (ru) 2011-02-10
EP2102161A2 (en) 2009-09-23
CA2672256A1 (en) 2008-06-19
KR20090090379A (ko) 2009-08-25
MX2009006266A (es) 2009-06-22
ATE556055T1 (de) 2012-05-15
NZ577639A (en) 2012-01-12
WO2008072079A2 (en) 2008-06-19
AU2007331199A1 (en) 2008-06-19
BRPI0720757A2 (pt) 2014-01-14
US20080177077A1 (en) 2008-07-24
JP2008231090A (ja) 2008-10-02
CA2672256C (en) 2011-08-30
EP2102161B1 (en) 2012-05-02
WO2008072079A3 (en) 2008-08-07
ZA200903981B (en) 2010-08-25
IL199239A0 (en) 2010-03-28

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