CO5080803A1 - Proceso de preparacion de 4-substituido-1h-indol-3-glioxami- das - Google Patents
Proceso de preparacion de 4-substituido-1h-indol-3-glioxami- dasInfo
- Publication number
- CO5080803A1 CO5080803A1 CO99022895A CO99022895A CO5080803A1 CO 5080803 A1 CO5080803 A1 CO 5080803A1 CO 99022895 A CO99022895 A CO 99022895A CO 99022895 A CO99022895 A CO 99022895A CO 5080803 A1 CO5080803 A1 CO 5080803A1
- Authority
- CO
- Colombia
- Prior art keywords
- formula
- compound
- jpeg
- mfi
- emi file
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/22—Radicals 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
-
- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Indole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un proceso de preparación de un compuesto de la fórmula I o una sal o prodroga derivada del mismo farmacéuticamente aceptable<EMI FILE="99022895_1" ID="1" IMF=JPEG >En donde:R1 es seleccionado del grupo que consiste de alquilo C7-C20;<EMI FILE="99022895_2" ID="2" IMF=JPEG >donde;R10 es seleccionado del grupo que consiste de halo, alquilo C1-C10, alcoxi C1-C10, -S-(aquil C1-C10) y halo alquilo C1-C10 y t es un entero entre 0 y 5 ambos incluidos; R2 es seleccionado del grupo que consiste de hidrógeno, halo, alquilo C1-C3, cicloalquilo C3-C4, cicloalquenilo C3-C4, -O-(alquil C1-C2), -S-(alquilo C1-C2), aril, ariloxi, y HET corresponde a un anillo heterocíclico que incluye piridina, pirazina, pirimidina, piridazina, pirazol, furano, tiofeno, tiofeno, tiazol, isotiazol, oxadiazol, imidazol, triazol y tetrazol;R4 es seleccionado del grupo que consiste de -CO2H, -SO3H, y -P(O)(OH)2 o una sal o prodroga derivadas del mismo; yR5 es seleccionado del grupo que consiste de hidrógeno, alquilo (C1-C6), alcoxi (C1-C6), halo alcoxi(C1-C6), halo alquil (C1-C6), bromo, cloro, flúor, yodo y arilo;Proceso que comprende los siguientes pasos:a) Halogenación de un compuesto de fórmula X<EMI FILE="99022895_3" ID="3" IMF=JPEG >En donde R8 es alquil (C1-C6), arilo o HET, en donde HET corresponde a un anillo heterocíclico que incluye piridina, pirazina, pirimidina, piridazina, pirrol, pirazol, furano, tiofeno, tiazol, isotiazol, oxadiazol, tiadiazol, imidazol, triazol y tetrazol;Con SO2Cl2 para formar un compuesto de fórmula IX<EMI FILE="99022895_4" ID="4" IMF=JPEG >b) Hidrolización y descarboxilación de un compuesto de fórmula IX<EMI FILE="99022895_5" ID="5" IMF=JPEG >- 2 -- 2 -Para formar un compuesto de fórmula VIII<EMI FILE="99022895_6" ID="6" IMF=JPEG >c) Alquilación de un compuesto de fórmula VII<EMI FILE="99022895_7" ID="7" IMF=JPEG >Con un compuesto de fórmula VIII<EMI FILE="99022895_8" ID="8" IMF=JPEG >Para formar un compuesto de fórmula VI<EMI FILE="99022895_9" ID="9" IMF=JPEG >d) Aminación y deshidratación de un compuesto de fórmula VI<EMI FILE="99022895_10" ID="10" IMF=JPEG >Con una amina de la fórmula R1NH2 en presencia de un solvente que formar un azeótropo con agua para formar un compuesto de formula V<EMI FILE="99022895_11" ID="11" IMF=JPEG >e) Oxidación de un compuesto de fórmula V<EMI FILE="99022895_12" ID="12" IMF=JPEG >Por el calentamiento por una base y un reactivo sulfinilante de la fórmula RSOX donde R es alquilo-( C1-C6) o arilo y X es alcoxi (C1-C6), halo, o -OCO2 alquilo(C1-C6) para formar un compuesto de fórmula IV<EMI FILE="99022895_13" ID="13" IMF=JPEG >f) Alquilación de un compuesto de fórmula IV<EMI FILE="99022895_14" ID="14" IMF=JPEG >con un agente alquilante de la fórmula XCH2R4a donde X es un grupo saliente y R4a es -CO2R4b , -SO3R4b , -P(O)(OR4b)2, o -P(O)(OR4b)H, donde R4b es un grupo protector ácido, para formar un compuesto de fórmula III<EMI FILE="99022895_15" ID="15" IMF=JPEG >g) Reacción de un compuesto de fórmula III<EMI FILE="99022895_16" ID="16" IMF=JPEG >con cloruro de oxalil y amoniaco para formar un compuesto de fórmula II<EMI FILE="99022895_17" ID="17" IMF=JPEG >h) Opcionalmente, hidrolización de un compuesto de fórmula II<EMI FILE="99022895_18" ID="18" IMF=JPEG >Para formar un compuesto de fórmula I; yi) Opcionalmente, salificación de un compuesto de fórmula I.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8211098P | 1998-04-17 | 1998-04-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5080803A1 true CO5080803A1 (es) | 2001-09-25 |
Family
ID=22169126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO99022895A CO5080803A1 (es) | 1998-04-17 | 1999-04-16 | Proceso de preparacion de 4-substituido-1h-indol-3-glioxami- das |
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6407261B1 (en) | 1998-04-17 | 2002-06-18 | Eli Lilly And Company | Process for preparing 4-hdyroxy indole, indazole and carbazole compounds |
| AU3563299A (en) * | 1998-04-17 | 1999-11-08 | Eli Lilly And Company | Process for preparing 4-hydroxy 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 |
| CN102413825A (zh) | 2009-04-29 | 2012-04-11 | 阿马里纳股份公司 | 含有epa和心血管剂的药物组合物以及使用其的方法 |
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW383302B (en) * | 1994-04-01 | 2000-03-01 | Lilly Co Eli | 1H-indole-3-glyoxylamide sPLA2 inhibitors |
| AU3563299A (en) * | 1998-04-17 | 1999-11-08 | Eli Lilly And Company | Process for preparing 4-hydroxy indole, indazole and carbazole compounds |
-
1999
- 1999-04-14 DZ DZ990070A patent/DZ2770A1/xx active
- 1999-04-15 CA CA002326515A patent/CA2326515A1/en not_active Abandoned
- 1999-04-15 HU HU0101344A patent/HUP0101344A3/hu unknown
- 1999-04-15 IL IL13882799A patent/IL138827A0/xx unknown
- 1999-04-15 SK SK1537-2000A patent/SK15372000A3/sk unknown
- 1999-04-15 US US09/647,471 patent/US6265591B1/en not_active Expired - Fee Related
- 1999-04-15 PE PE1999000312A patent/PE20000430A1/es not_active Application Discontinuation
- 1999-04-15 JP JP2000544641A patent/JP2002512225A/ja not_active Withdrawn
- 1999-04-15 WO PCT/US1999/008332 patent/WO1999054300A1/en not_active Application Discontinuation
- 1999-04-15 SV SV1999000043A patent/SV1999000043A/es not_active Application Discontinuation
- 1999-04-15 AU AU35648/99A patent/AU750368B2/en not_active Ceased
- 1999-04-15 TR TR2000/02999T patent/TR200002999T2/xx unknown
- 1999-04-15 NZ NZ507175A patent/NZ507175A/xx unknown
- 1999-04-15 AR ARP990101753A patent/AR015767A1/es not_active Application Discontinuation
- 1999-04-15 EG EG104099D patent/EG22139A/xx active
- 1999-04-15 BR BR9909697-8A patent/BR9909697A/pt not_active IP Right Cessation
- 1999-04-15 CN CN99807248A patent/CN1305459A/zh active Pending
- 1999-04-15 PL PL99343487A patent/PL343487A1/xx not_active Application Discontinuation
- 1999-04-15 KR KR1020007011468A patent/KR20010042741A/ko not_active Application Discontinuation
- 1999-04-15 ID IDW20002058A patent/ID26021A/id unknown
- 1999-04-15 EP EP99917556A patent/EP1071663A4/en not_active Withdrawn
- 1999-04-15 EA EA200001076A patent/EA003582B1/ru not_active IP Right Cessation
- 1999-04-16 CO CO99022895A patent/CO5080803A1/es unknown
-
2000
- 2000-09-29 ZA ZA200005294A patent/ZA200005294B/en unknown
- 2000-10-13 NO NO20005148A patent/NO20005148L/no not_active Application Discontinuation
- 2000-10-17 HR HR20000685A patent/HRP20000685A2/hr not_active Application Discontinuation
-
2002
- 2002-01-23 HK HK02100522.5A patent/HK1039120A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP1071663A4 (en) | 2002-06-19 |
| BR9909697A (pt) | 2000-12-19 |
| NZ507175A (en) | 2002-12-20 |
| PE20000430A1 (es) | 2000-05-24 |
| US6265591B1 (en) | 2001-07-24 |
| NO20005148D0 (no) | 2000-10-13 |
| PL343487A1 (en) | 2001-08-27 |
| EG22139A (en) | 2002-08-30 |
| CN1305459A (zh) | 2001-07-25 |
| ID26021A (id) | 2000-11-16 |
| EA003582B1 (ru) | 2003-06-26 |
| NO20005148L (no) | 2000-11-09 |
| EA200001076A1 (ru) | 2001-04-23 |
| WO1999054300A1 (en) | 1999-10-28 |
| KR20010042741A (ko) | 2001-05-25 |
| EP1071663A1 (en) | 2001-01-31 |
| JP2002512225A (ja) | 2002-04-23 |
| AU3564899A (en) | 1999-11-08 |
| HUP0101344A2 (hu) | 2001-09-28 |
| HUP0101344A3 (en) | 2002-12-28 |
| AU750368B2 (en) | 2002-07-18 |
| CA2326515A1 (en) | 1999-10-28 |
| HK1039120A1 (zh) | 2002-04-12 |
| HRP20000685A2 (en) | 2001-10-31 |
| AR015767A1 (es) | 2001-05-16 |
| DZ2770A1 (fr) | 2003-12-01 |
| SV1999000043A (es) | 2000-05-02 |
| SK15372000A3 (sk) | 2001-08-06 |
| TR200002999T2 (tr) | 2001-01-22 |
| IL138827A0 (en) | 2001-10-31 |
| ZA200005294B (en) | 2001-10-01 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES8605500A1 (es) | Procedimiento para preparar derivados de acidos fenilaceticos. | |
| MY109743A (en) | Pyrimidine derivatives. | |
| PT87329A (pt) | Process for preparing a stabilized hydrogen peroxide solution for disinfecting contact lens | |
| CA2331873A1 (en) | Fumagillol derivatives and processes for preparing the same | |
| WO2007105253B1 (en) | PREPARATION OF (1-OXA- OR l-THIA-)3- CEPHEM DERIVATIVES | |
| PL354611A1 (en) | Process for preparing 4-trifluoromethylsulphinylpyrazole derivative | |
| CO5080803A1 (es) | Proceso de preparacion de 4-substituido-1h-indol-3-glioxami- das | |
| US12054489B2 (en) | Substituted amidrazones as intermediates in the process for preparing soluble guanylate cyclase stimulators | |
| AR053722A2 (es) | Procedimiento para preparar secretagogos de hormonas del crecimiento y poliformo de los compuestos obtenidos | |
| IE781926L (en) | Peptides analgesics | |
| CO5021230A1 (es) | Proceso de preparacion de 4-substituido-1h-indol-3- glioxamidas | |
| ES2059454T3 (es) | Composicion de antibiotico soluble en agua y sales solubles en agua de nuevos compuestos de cefem. | |
| DE3476066D1 (en) | Salt free phosphobetaines | |
| ES9000003A1 (es) | Procedimiento de producir agentes terapeuticos y profilacticos para ulceras pepticas | |
| DE69405300D1 (de) | Verfahren zur Herstellung von Cephalosporinverbindungen aus reaktiven organischen Säurederivaten | |
| HUT37431A (en) | Process for the production of imidazo /1,2-c/pyrimidines and of their salts,as well as of therapeutic preparations containing these compounds as agent | |
| DE60316459D1 (de) | Verfahren zur herstellung von ceftiofur | |
| ES446126A1 (es) | Procedimiento para preparar 2-(fenoxialquiltio) imidazoles. | |
| ATE354540T1 (de) | Nonaboratzusammensetzung und ihre herstellung | |
| ES2004809A6 (es) | Procedimiento de obtencion de nuevas 1-(2-(fenilmetil)fenil)piperazinas | |
| ES2188482T3 (es) | Procedimiento para la preparacion de indoles acilados en la posicion 3. | |
| EP0223512A3 (en) | 2-pyridylacetic acid derivative, preparation process thereof and pharmaceutical composition containing the same | |
| ECSP992922A (es) | Proceso para preparar 4- sustituidas- 1h- indola-3- glioxamidas | |
| US5053500A (en) | Intermediates for the preparation of beta-lactam antibiotics | |
| GB997166A (en) | N-phenylpiperazine derivatives |