PE20000430A1 - Proceso para preparar 4-sustituido-1h-indol-3-glioxamidas - Google Patents

Proceso para preparar 4-sustituido-1h-indol-3-glioxamidas

Info

Publication number
PE20000430A1
PE20000430A1 PE1999000312A PE00031299A PE20000430A1 PE 20000430 A1 PE20000430 A1 PE 20000430A1 PE 1999000312 A PE1999000312 A PE 1999000312A PE 00031299 A PE00031299 A PE 00031299A PE 20000430 A1 PE20000430 A1 PE 20000430A1
Authority
PE
Peru
Prior art keywords
alkyl
compound
halo
forming
group
Prior art date
Application number
PE1999000312A
Other languages
English (en)
Inventor
Benjamin Alan Anderson
Nancy Kay Harn
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20000430A1 publication Critical patent/PE20000430A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/22Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an aralkyl radical attached to the ring nitrogen atom
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

SE REFIERE A UN PROCEDIMIENTO PARA PREPARAR 1H-INDOL-3-GLIOXAMIDAS DE FORMULA I, DONDE R1 ES ALQUILO C7-C20, GRUPO a, b, c; R10 ES HALO, ALQUILO C1-C10, ENTRE OTROS; t ES 0-5; R2 ES H, HALO, ALQUILO C1-C3, ENTRE OTROS; R4 ES -CO2H, SO3H, PO(OH)2; R5 ES H, ALQUILO C1-C6, ALCOXI C1-C6, ENTRE OTROS; QUE COMPRENDE HALOGENAR R8-O-C(=O)-CH2-C(=O)-R2; R8 ES ALQUILO C1-C6, ARILO, HET; CON SO2Cl2 Y FORMAR R8-O-(C=O)-CH(Cl)-C(=O)-R2; LUEGO HIDROLIZAR, DESCARBOXILAR Y FORMAR Cl-CH2-C(=O)-R2; ALQUILIZAR UN COMPUESTO VII CON Cl-CH2-C(=O)-R2; PARA FORMAR UN COMPUESTO VI LUEGO AMINAR Y DESHIDRATAR CON UNA AMINA R1NH2, EN PRESENCIA DE UN SOLVENTE QUE FORMA UN AZEOTROPO EN AGUA PARA FORMAR UN COMPUESTO V; LUEGO OXIDAR CALENTANDO CON UNA BASE Y UN REACTIVO SULFINIZANTE RSOX; R ES -ALQUILO C1-C6, ARILO; X ES -ALCOXI C1-C6, HALO, -OCO2(ALQUILO C1-C6) Y FORMAR UN COMPUESTO IV; LUEGO ALQUILAR CON XCH2R4a; X ES UN GRUPO SALIENTE, R4a ES -CO2R4b, -SO3R4b, -P(O)(OR4b)2, -P(O)(OR4b)H; R4b ES UN GRUPO ACIDO PROTECTOR Y FORMAR UN GRUPO III, QUE REACCIONA CON CLORURO DE OXALILO, AMONIACO Y FORMAR UN COMPUESTO II; LUEGO HIDROLIZAR Y FORMAR EL COMPUESTO I EL QUE ES UN INHIBIDOR DE LA LIBERACION DE ACIDOS GRASOS OCASIONADA POR sPLA2 Y PUEDE SER UTIL PARA TRATAR SHOCK SEPTICO, PANCREATITIS, TRAUMA
PE1999000312A 1998-04-17 1999-04-15 Proceso para preparar 4-sustituido-1h-indol-3-glioxamidas PE20000430A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US8211098P 1998-04-17 1998-04-17

Publications (1)

Publication Number Publication Date
PE20000430A1 true PE20000430A1 (es) 2000-05-24

Family

ID=22169126

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1999000312A PE20000430A1 (es) 1998-04-17 1999-04-15 Proceso para preparar 4-sustituido-1h-indol-3-glioxamidas

Country Status (27)

Country Link
US (1) US6265591B1 (es)
EP (1) EP1071663A4 (es)
JP (1) JP2002512225A (es)
KR (1) KR20010042741A (es)
CN (1) CN1305459A (es)
AR (1) AR015767A1 (es)
AU (1) AU750368B2 (es)
BR (1) BR9909697A (es)
CA (1) CA2326515A1 (es)
CO (1) CO5080803A1 (es)
DZ (1) DZ2770A1 (es)
EA (1) EA003582B1 (es)
EG (1) EG22139A (es)
HK (1) HK1039120A1 (es)
HR (1) HRP20000685A2 (es)
HU (1) HUP0101344A3 (es)
ID (1) ID26021A (es)
IL (1) IL138827A0 (es)
NO (1) NO20005148L (es)
NZ (1) NZ507175A (es)
PE (1) PE20000430A1 (es)
PL (1) PL343487A1 (es)
SK (1) SK15372000A3 (es)
SV (1) SV1999000043A (es)
TR (1) TR200002999T2 (es)
WO (1) WO1999054300A1 (es)
ZA (1) ZA200005294B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1071661A4 (en) * 1998-04-17 2001-08-22 Lilly Co Eli METHOD FOR PRODUCING 4-HYDROXYINDOL, INDAZOL AND CARBAZOL COMPOUNDS
US6407261B1 (en) 1998-04-17 2002-06-18 Eli Lilly And Company Process for preparing 4-hdyroxy indole, indazole and carbazole compounds
DE19962300A1 (de) * 1999-12-23 2001-06-28 Asta Medica Ag Substituierte N-Benzyl-Indol-3-yl-glyoxylsäure-Derivate mit Antitumorwirkung
US20030225149A1 (en) * 2002-04-30 2003-12-04 Blazecka Peter G. Process for preparing highly functionalized gamma-butyrolactams and gamma-amino acids
NZ624963A (en) 2009-04-29 2016-07-29 Amarin Pharmaceuticals Ie Ltd Pharmaceutical compositions comprising epa and a cardiovascular agent and methods of using the same
AR088377A1 (es) 2011-10-20 2014-05-28 Siena Biotech Spa Proceso para la preparacion de 6-cloro-2,3,4,9-tetrahidro-1h-carbazol-1-carboxamida y compuestos intermedios de esta

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY112897A (en) 1994-04-01 2001-10-31 Lilly Co Eli Ih-indole-3-glyoxylamide spla2 inhibitors
EP1071661A4 (en) * 1998-04-17 2001-08-22 Lilly Co Eli METHOD FOR PRODUCING 4-HYDROXYINDOL, INDAZOL AND CARBAZOL COMPOUNDS

Also Published As

Publication number Publication date
ZA200005294B (en) 2001-10-01
HRP20000685A2 (en) 2001-10-31
SV1999000043A (es) 2000-05-02
CA2326515A1 (en) 1999-10-28
EG22139A (en) 2002-08-30
WO1999054300A1 (en) 1999-10-28
EA200001076A1 (ru) 2001-04-23
CN1305459A (zh) 2001-07-25
PL343487A1 (en) 2001-08-27
EP1071663A1 (en) 2001-01-31
AU3564899A (en) 1999-11-08
BR9909697A (pt) 2000-12-19
NO20005148D0 (no) 2000-10-13
EA003582B1 (ru) 2003-06-26
AR015767A1 (es) 2001-05-16
AU750368B2 (en) 2002-07-18
IL138827A0 (en) 2001-10-31
TR200002999T2 (tr) 2001-01-22
KR20010042741A (ko) 2001-05-25
DZ2770A1 (fr) 2003-12-01
NO20005148L (no) 2000-11-09
EP1071663A4 (en) 2002-06-19
HUP0101344A2 (hu) 2001-09-28
CO5080803A1 (es) 2001-09-25
NZ507175A (en) 2002-12-20
US6265591B1 (en) 2001-07-24
HUP0101344A3 (en) 2002-12-28
ID26021A (id) 2000-11-16
JP2002512225A (ja) 2002-04-23
HK1039120A1 (zh) 2002-04-12
SK15372000A3 (sk) 2001-08-06

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Legal Events

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FG Grant, registration
FD Application declared void or lapsed