PE16799A1 - Procedimiento para la sintesis de benzotiofenos - Google Patents
Procedimiento para la sintesis de benzotiofenosInfo
- Publication number
- PE16799A1 PE16799A1 PE1997001035A PE00103597A PE16799A1 PE 16799 A1 PE16799 A1 PE 16799A1 PE 1997001035 A PE1997001035 A PE 1997001035A PE 00103597 A PE00103597 A PE 00103597A PE 16799 A1 PE16799 A1 PE 16799A1
- Authority
- PE
- Peru
- Prior art keywords
- compound
- formula
- thiophene
- benzo
- hydroxy
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 abstract 2
- KFZMGEQAYNKOFK-YZRHJBSPSA-N (214C)propan-2-ol Chemical compound [14CH](C)(C)O KFZMGEQAYNKOFK-YZRHJBSPSA-N 0.000 abstract 1
- OMPJBNCRMGITSC-UHFFFAOYSA-N Benzoylperoxide Chemical compound C=1C=CC=CC=1C(=O)OOC(=O)C1=CC=CC=C1 OMPJBNCRMGITSC-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 230000001351 cycling effect Effects 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 abstract 1
- 230000008521 reorganization Effects 0.000 abstract 1
- YXFVVABEGXRONW-CNRUNOGKSA-N tritiomethylbenzene Chemical compound [3H]CC1=CC=CC=C1 YXFVVABEGXRONW-CNRUNOGKSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/56—Radicals substituted by oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
CARACTERIZADO PORQUE COMPRENDE LA CICLIZACION DEL COMPUESTO DE FORMULA (II), EN DONDE: R ES ALQUILO C1-C6, DE PREFERENCIA METILO, EN PRESENCIA DE ACIDO METANOSULFONICO, ADEMAS DE TOLUENO, HEPTANO e ISOPROPANOL, DICHA REACCION SE LLEVA A CABO A UNA TEMPERATURA APROXIMADA DE 70�C A 90�C; OBTENIENDOSE EL COMPUESTO DE FORMULA (Ib), QUE POR REORDENAMIENTO FORMA EL COMPUESTO DE FORMULA (I) QUE PREFERENTEMENTE ES 6-METOXI-2-(4-METOXIFENIL)BENZO[b]TIOFENO, EL CUAL SE PUEDE CONVERTIR POSTERIORMENTE EN 6-HIDROXI-2-(4-HIDROXIFENIL)-3-[4-(2-PIPERIDINOETOXI)BENZOIL]BENZO[b]TIOFENO CONOCIDO COMO RALOXIFENO, QUE ES UN MODULADOR SELECTIVO DEL RECEPTOR DE ESTROGENO. ESTE PROCEDIMIENTO MEJORA EL RENDIMIENTO DE DICHO PRINCIPIO ACTIVO A ESCALA INDUSTRIAL
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3118196P | 1996-11-19 | 1996-11-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE16799A1 true PE16799A1 (es) | 1999-02-19 |
Family
ID=21858059
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1997001035A PE16799A1 (es) | 1996-11-19 | 1997-11-14 | Procedimiento para la sintesis de benzotiofenos |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US5969157A (es) |
| EP (1) | EP0842930B1 (es) |
| JP (1) | JP2001504497A (es) |
| KR (1) | KR20000053333A (es) |
| CN (1) | CN1130357C (es) |
| AR (1) | AR010615A1 (es) |
| AT (1) | ATE217620T1 (es) |
| AU (1) | AU726401B2 (es) |
| BR (1) | BR9712773A (es) |
| CA (1) | CA2271922A1 (es) |
| CO (1) | CO4920247A1 (es) |
| DE (1) | DE69712590T2 (es) |
| DK (1) | DK0842930T3 (es) |
| ES (1) | ES2173399T3 (es) |
| HU (1) | HUP9904510A3 (es) |
| ID (1) | ID18917A (es) |
| IL (1) | IL129868A (es) |
| PE (1) | PE16799A1 (es) |
| PT (1) | PT842930E (es) |
| SI (1) | SI0842930T1 (es) |
| TW (1) | TW461888B (es) |
| WO (1) | WO1998022456A1 (es) |
| ZA (1) | ZA9710262B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001009116A2 (en) * | 1999-07-29 | 2001-02-08 | Eli Lilly And Company | A NOVEL CRYSTALLINE FORM OF 6-HYDROXY-3- (4-[2-(PIPERIDIN-1-YL) ETHOXY]PHENOXY)- 2-(4-METHOXYPHENYL)BENZO[b]THIOPHENE HYDROCHLORIDE |
| US6921827B2 (en) * | 2000-11-27 | 2005-07-26 | Eli Lilly And Company | Process for preparing 3-aryl-benzo{b} thiophenes |
| US8323903B2 (en) | 2001-10-12 | 2012-12-04 | Life Technologies Corporation | Antibody complexes and methods for immunolabeling |
| US20050069962A1 (en) | 2001-10-12 | 2005-03-31 | Archer Robert M | Antibody complexes and methods for immunolabeling |
| CA2492631C (en) * | 2002-05-31 | 2013-03-12 | Genetic Technologies Limited | Maternal antibodies as fetal cell markers to identify and enrich fetal cells from maternal blood |
| US7964734B2 (en) | 2002-09-30 | 2011-06-21 | A/S Gea Farmaceutisk Fabrik | Raloxifene acid addition salts and/or solvates thereof, improved method for purification of said raloxifene acid addition salts and/or solvates thereof and pharmaceutical compositions comprising these |
| AU2004217872B2 (en) * | 2003-03-05 | 2010-03-25 | Genetic Technologies Limited | Identification of fetal DNA and fetal cell markers in maternal plasma or serum |
| WO2008047105A1 (en) | 2006-10-17 | 2008-04-24 | Cipla Limited | Crystalline form of benzothiophene compound and process for preparation thereof |
| AU2010239131A1 (en) | 2009-04-21 | 2011-11-17 | Genetic Technologies Limited | Methods for obtaining fetal genetic material |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4133814A (en) * | 1975-10-28 | 1979-01-09 | Eli Lilly And Company | 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents |
| AU509682B2 (en) * | 1975-10-28 | 1980-05-22 | Eli Lilly And Company | 2-Aroyl-3-Phenylbenzothiophene Derivatives |
| AT364852B (de) * | 1977-11-05 | 1981-11-25 | Thomae Gmbh Dr K | Verfahren zur herstellung von kondensierten isothiazol-3(2h)-on-1,1-dioxiden und von deren salzen |
| US4436748A (en) * | 1980-10-20 | 1984-03-13 | Hoechst-Roussel Pharmaceuticals Inc. | Benzo[b]thiophenes |
| IL65378A (en) * | 1981-04-03 | 1986-02-28 | Lilly Co Eli | Process for preparing 3-(4-aminoethoxybenzoyl)benzo-(b)thiophenes |
| US4418068A (en) * | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
| US4380635A (en) * | 1981-04-03 | 1983-04-19 | Eli Lilly And Company | Synthesis of acylated benzothiophenes |
| US4544746A (en) * | 1982-05-17 | 1985-10-01 | Ciba-Geigy Corporation | Process for preparing 2-anilinoacridone |
| JP3157882B2 (ja) * | 1991-11-15 | 2001-04-16 | 帝国臓器製薬株式会社 | 新規なベンゾチオフエン誘導体 |
| DE4204969A1 (de) * | 1992-02-19 | 1993-08-26 | Basf Ag | Verfahren zur herstellung von benzo(b)thiophenen |
| US5466810A (en) * | 1994-06-10 | 1995-11-14 | Eli Lilly And Company | 2-amino-3-aroyl-benzo[β]thiophenes and methods for preparing and using same to produce 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-aminoethoxy)-benzoyl]benzo[β]thiophenes |
| DE4423893C2 (de) * | 1994-07-07 | 1996-09-05 | Freudenberg Carl Fa | Flachdichtung mit flexibler Leiterplatte |
| US5523416A (en) * | 1994-07-22 | 1996-06-04 | Eli Lilly And Company | Process for preparing 3-(4-aminoethoxy-benzoyl) benzo (B)-thiophenes |
| US5552401A (en) * | 1995-02-28 | 1996-09-03 | Eli Lilly And Company | 2-benzyl-3-arylbenzothiophenes |
| US5614639A (en) * | 1995-03-31 | 1997-03-25 | Eli Lilly And Company | Process for preparing 2-substituted benzo[b]thiophene compounds and intermediates thereof |
| US5606075A (en) * | 1995-06-07 | 1997-02-25 | Eli Lilly And Company | Process for the synthesis of benzo[b]thiophenes |
| US5606076A (en) * | 1995-06-07 | 1997-02-25 | Eli Lilly And Company | Process for the synthesis of benzo[b]thiophenes |
-
1997
- 1997-11-13 ZA ZA9710262A patent/ZA9710262B/xx unknown
- 1997-11-14 AU AU54622/98A patent/AU726401B2/en not_active Ceased
- 1997-11-14 PT PT97309186T patent/PT842930E/pt unknown
- 1997-11-14 JP JP52400398A patent/JP2001504497A/ja active Pending
- 1997-11-14 PE PE1997001035A patent/PE16799A1/es not_active Application Discontinuation
- 1997-11-14 CA CA002271922A patent/CA2271922A1/en not_active Abandoned
- 1997-11-14 KR KR1019990704344A patent/KR20000053333A/ko not_active Ceased
- 1997-11-14 WO PCT/US1997/021820 patent/WO1998022456A1/en not_active Ceased
- 1997-11-14 ES ES97309186T patent/ES2173399T3/es not_active Expired - Lifetime
- 1997-11-14 BR BR9712773-6A patent/BR9712773A/pt unknown
- 1997-11-14 AT AT97309186T patent/ATE217620T1/de active
- 1997-11-14 SI SI9730342T patent/SI0842930T1/xx unknown
- 1997-11-14 DK DK97309186T patent/DK0842930T3/da active
- 1997-11-14 CN CN97199842A patent/CN1130357C/zh not_active Expired - Fee Related
- 1997-11-14 IL IL12986897A patent/IL129868A/en not_active IP Right Cessation
- 1997-11-14 EP EP97309186A patent/EP0842930B1/en not_active Expired - Lifetime
- 1997-11-14 DE DE69712590T patent/DE69712590T2/de not_active Expired - Lifetime
- 1997-11-14 HU HU9904510A patent/HUP9904510A3/hu unknown
- 1997-11-14 CO CO97067013A patent/CO4920247A1/es unknown
- 1997-11-17 ID IDP973692A patent/ID18917A/id unknown
- 1997-11-17 AR ARP970105369A patent/AR010615A1/es active IP Right Grant
- 1997-11-18 US US08/972,783 patent/US5969157A/en not_active Expired - Lifetime
- 1997-11-22 TW TW086117219A patent/TW461888B/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| WO1998022456A1 (en) | 1998-05-28 |
| CN1237968A (zh) | 1999-12-08 |
| DK0842930T3 (da) | 2002-07-15 |
| CO4920247A1 (es) | 2000-05-29 |
| EP0842930B1 (en) | 2002-05-15 |
| US5969157A (en) | 1999-10-19 |
| DE69712590T2 (de) | 2002-10-31 |
| DE69712590D1 (de) | 2002-06-20 |
| IL129868A (en) | 2002-09-12 |
| ID18917A (id) | 1998-05-20 |
| JP2001504497A (ja) | 2001-04-03 |
| AU726401B2 (en) | 2000-11-09 |
| PT842930E (pt) | 2002-08-30 |
| EP0842930A1 (en) | 1998-05-20 |
| IL129868A0 (en) | 2000-02-29 |
| AU5462298A (en) | 1998-06-10 |
| BR9712773A (pt) | 1999-10-26 |
| HUP9904510A2 (hu) | 2000-05-28 |
| CN1130357C (zh) | 2003-12-10 |
| TW461888B (en) | 2001-11-01 |
| KR20000053333A (ko) | 2000-08-25 |
| ZA9710262B (en) | 1999-05-13 |
| AR010615A1 (es) | 2000-06-28 |
| ATE217620T1 (de) | 2002-06-15 |
| CA2271922A1 (en) | 1998-05-28 |
| SI0842930T1 (en) | 2002-10-31 |
| HUP9904510A3 (en) | 2000-08-28 |
| ES2173399T3 (es) | 2002-10-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |