ES2532903T3 - Métodos y compuestos para la preparación de compuestos orgánicos biológicamente activos monofluorometilados - Google Patents
Métodos y compuestos para la preparación de compuestos orgánicos biológicamente activos monofluorometilados Download PDFInfo
- Publication number
- ES2532903T3 ES2532903T3 ES11727731.9T ES11727731T ES2532903T3 ES 2532903 T3 ES2532903 T3 ES 2532903T3 ES 11727731 T ES11727731 T ES 11727731T ES 2532903 T3 ES2532903 T3 ES 2532903T3
- Authority
- ES
- Spain
- Prior art keywords
- compounds
- biologically active
- monofluoromethylated
- preparation
- active organic
- Prior art date
- Legal status (The legal status 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 status listed.)
- Active
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 150000002894 organic compounds Chemical class 0.000 title abstract 2
- 229910014263 BrF3 Inorganic materials 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical group CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 229910019142 PO4 Inorganic materials 0.000 abstract 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 abstract 1
- UQSQSQZYBQSBJZ-UHFFFAOYSA-M fluorosulfonate Chemical compound [O-]S(F)(=O)=O UQSQSQZYBQSBJZ-UHFFFAOYSA-M 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 abstract 1
- 239000010452 phosphate Substances 0.000 abstract 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical group [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 abstract 1
- FQFKTKUFHWNTBN-UHFFFAOYSA-N trifluoro-$l^{3}-bromane Chemical compound FBr(F)F FQFKTKUFHWNTBN-UHFFFAOYSA-N 0.000 abstract 1
- IGELFKKMDLGCJO-UHFFFAOYSA-N xenon difluoride Chemical compound F[Xe]F IGELFKKMDLGCJO-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J75/00—Processes for the preparation of steroids in general
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
- C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Un método para preparar un compuesto orgánico biológicamente activo que contiene un resto "CH2F", método que comprende las etapas de: hacer reaccionar un compuesto de fórmula R*-SH con ácido X-acético para producir un intermedio de fórmula R*-S-CH2COOH; fluorodescarboxilar el intermedio de fórmula R*-S-CH2COOH con un reactivo seleccionado de un grupo que consiste en XeF2 y BrF3 para producir un compuesto de fórmula R*-S-CH2F, en donde: R*SH es una molécula multifuncional orgánica; y X es halógeno, triflato, mesilato, un fluorosulfonato o un fosfato.
Description
Claims (1)
-
imagen1 imagen2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PT105138A PT105138B (pt) | 2010-06-01 | 2010-06-01 | Método para a preparação de compostos orgânicos monofluorometilados biologicamente activos |
| PT513810 | 2010-06-01 | ||
| PCT/GB2011/000835 WO2011151625A1 (en) | 2010-06-01 | 2011-06-01 | Methods and compounds for the preparation of monofluoromethylated biologically active organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2532903T3 true ES2532903T3 (es) | 2015-04-01 |
Family
ID=44627526
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11727731.9T Active ES2532903T3 (es) | 2010-06-01 | 2011-06-01 | Métodos y compuestos para la preparación de compuestos orgánicos biológicamente activos monofluorometilados |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20130072698A1 (es) |
| EP (1) | EP2576584B1 (es) |
| CN (1) | CN103038244A (es) |
| ES (1) | ES2532903T3 (es) |
| PT (1) | PT105138B (es) |
| WO (1) | WO2011151625A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT105139B (pt) * | 2010-06-01 | 2013-01-29 | Hovione Farmaciencia S A | Método para a monofluorometilação de substratos orgânicos para preparação de compostos orgânicos biologicamente activos |
| PT105723B (pt) | 2011-05-26 | 2014-03-24 | Hovione Farmaci Ncia S A | Método para a preparação de compostos orgânicos biologicamente activos |
| CN103073613B (zh) * | 2012-12-31 | 2016-04-13 | 浙江工业大学 | 一种氟替卡松衍生物的合成方法 |
| CN111662353A (zh) * | 2019-03-05 | 2020-09-15 | 上海谷森医药有限公司 | 一种糠酸氟替卡松晶型1的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3399179A (en) * | 1963-01-03 | 1968-08-27 | Aerojet General Co | Decarboxylation of organic carboxylic acids and acid salts with fluorine to form organic fluorine compounds |
| US4996371A (en) * | 1990-01-16 | 1991-02-26 | Boc, Inc. | Method for fluorodecarboxylation |
| PL309402A1 (en) * | 1992-12-24 | 1995-10-02 | Rhone Poulenc Rorer Ltd | Novel steroides |
| GB9418305D0 (en) * | 1994-09-10 | 1994-11-02 | Solvay Interox Ltd | Process for the introduction of fluoro substituents |
| CZ304043B6 (cs) * | 2000-08-05 | 2013-09-04 | Glaxo Group Limited | Estery steroidních thiokyselin |
| CN100549022C (zh) * | 2007-08-15 | 2009-10-14 | 湖南玉新药业有限公司 | 制备氟替卡松丙酸酯的方法 |
| PT105723B (pt) * | 2011-05-26 | 2014-03-24 | Hovione Farmaci Ncia S A | Método para a preparação de compostos orgânicos biologicamente activos |
-
2010
- 2010-06-01 PT PT105138A patent/PT105138B/pt not_active IP Right Cessation
-
2011
- 2011-06-01 ES ES11727731.9T patent/ES2532903T3/es active Active
- 2011-06-01 WO PCT/GB2011/000835 patent/WO2011151625A1/en not_active Ceased
- 2011-06-01 US US13/701,211 patent/US20130072698A1/en not_active Abandoned
- 2011-06-01 CN CN2011800377125A patent/CN103038244A/zh active Pending
- 2011-06-01 EP EP11727731.9A patent/EP2576584B1/en not_active Not-in-force
Also Published As
| Publication number | Publication date |
|---|---|
| PT105138A (pt) | 2011-12-02 |
| US20130072698A1 (en) | 2013-03-21 |
| CN103038244A (zh) | 2013-04-10 |
| PT105138B (pt) | 2012-11-06 |
| WO2011151625A1 (en) | 2011-12-08 |
| EP2576584A1 (en) | 2013-04-10 |
| EP2576584B1 (en) | 2015-01-07 |
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