MX2015017536A - Alquilacion con un alquil sulfonato de fluoroalquilo. - Google Patents
Alquilacion con un alquil sulfonato de fluoroalquilo.Info
- Publication number
- MX2015017536A MX2015017536A MX2015017536A MX2015017536A MX2015017536A MX 2015017536 A MX2015017536 A MX 2015017536A MX 2015017536 A MX2015017536 A MX 2015017536A MX 2015017536 A MX2015017536 A MX 2015017536A MX 2015017536 A MX2015017536 A MX 2015017536A
- Authority
- MX
- Mexico
- Prior art keywords
- alkyl
- preparing
- sulfonate
- fluoroalkyi
- reactants
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 title abstract 5
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 title abstract 4
- 230000029936 alkylation Effects 0.000 title 1
- 238000005804 alkylation reaction Methods 0.000 title 1
- 125000003709 fluoroalkyl group Chemical group 0.000 title 1
- 239000000376 reactant Substances 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 229960005167 everolimus Drugs 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000012038 nucleophile Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/26—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
- C07C303/28—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Immunology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención describe un procedimiento para preparar un compuesto químico que comprende la reacción de un nucleófilo con un alquil sulfonato de fluoroalquilo en presencia de una base de la fórmula NR1R2R3, en donde R1 y R2 son independientemente 2-metilpropilo o isopropilo y R3 es-CH(R4)(R5), en donde R4 y R5 son alquilos idénticos o diferentes que están opcionalmente conectados para formar un anillo. La invención también se refiere a un procedimiento para la preparación de un alquil sulfonato de fluoroalquilo. La invención además se refiere a un uso de la base en una reacción química que comprende un alquil sulfonato de fluoroalquilo. El proceso y los usos son apropiados para la preparación de compuestos químicos, reactivos o intermedios de los mismos, y en particular para la preparación de API o reactivos, como por ejemplo everolimus o reactivos para su preparación.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361837224P | 2013-06-20 | 2013-06-20 | |
| PCT/IB2014/062375 WO2014203185A1 (en) | 2013-06-20 | 2014-06-18 | Alkylation with an alkyl fluoroalkyl sulfonate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2015017536A true MX2015017536A (es) | 2016-04-26 |
Family
ID=51014598
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2015017536A MX2015017536A (es) | 2013-06-20 | 2014-06-18 | Alquilacion con un alquil sulfonato de fluoroalquilo. |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20160130280A1 (es) |
| EP (1) | EP3010926B1 (es) |
| JP (1) | JP6574173B2 (es) |
| KR (1) | KR20160021243A (es) |
| CN (2) | CN109651396B (es) |
| AU (1) | AU2014282831B2 (es) |
| BR (1) | BR112015029521A2 (es) |
| CA (1) | CA2911104A1 (es) |
| HK (1) | HK1219727A1 (es) |
| IL (1) | IL242413B (es) |
| MX (1) | MX2015017536A (es) |
| RU (1) | RU2691728C2 (es) |
| WO (1) | WO2014203185A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104592254B (zh) * | 2015-02-08 | 2016-07-13 | 福建省微生物研究所 | 依维莫司的合成方法 |
| CN104876944B (zh) * | 2015-05-13 | 2017-11-10 | 普济生物科技（台州）有限公司 | 一种依维莫司的制备方法 |
| EP3109250A1 (en) * | 2015-06-23 | 2016-12-28 | Synbias Pharma AG | Method for the synthesis of rapamycin derivatives |
| CN108047265A (zh) * | 2017-11-24 | 2018-05-18 | 成都海创药业有限公司 | 一种依维莫司中间体的制备纯化方法 |
| RU2716714C1 (ru) * | 2019-08-26 | 2020-03-16 | Закрытое Акционерное Общество "Биокад" | Новый способ получения эверолимуса |
| CZ308817B6 (cs) * | 2019-09-12 | 2021-06-09 | Ratiochem, s.r.o. | Způsob výroby Everolimu |
| JP2023028473A (ja) * | 2021-08-19 | 2023-03-03 | 日本マイクロバイオファーマ株式会社 | エベロリムスの製造方法 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9221220D0 (en) * | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| CZ292233B6 (cs) * | 1995-06-09 | 2003-08-13 | Novartis Ag | Deriváty rapamycinu a jejich použití jako léčiv |
| CN1235608A (zh) * | 1996-09-09 | 1999-11-17 | 美国家用产品公司 | 烷基化的雷帕霉素衍生物 |
| EP1571151B1 (en) | 2004-03-01 | 2008-12-24 | Terumo Kabushiki Kaisha | Process for production of O-alkylated rapamycin derivatives |
| JP4716280B2 (ja) * | 2004-03-01 | 2011-07-06 | テルモ株式会社 | Ｏ−アルキル化ラパマイシン誘導体の製造法 |
| ES2296516B1 (es) | 2006-04-27 | 2009-04-01 | Laboratorios Almirall S.A. | Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico. |
| TW200948361A (en) | 2008-05-26 | 2009-12-01 | Chunghwa Chemical Synthesis & Biotech Co Ltd | Method for synthesizing Biolimus A9 and the like and method for improving stability of the same |
| CN102127092B (zh) * | 2010-01-18 | 2013-04-17 | 东南大学 | 依维莫斯的制备 |
| EP2640730B1 (en) * | 2010-11-19 | 2019-08-07 | Biocon Limited | Processes for preparation of everolimus and intermediates thereof |
| WO2012103959A1 (en) * | 2011-02-04 | 2012-08-09 | Synthon Bv | Process for making everolimus |
-
2014
- 2014-06-18 CN CN201910054592.8A patent/CN109651396B/zh active Active
- 2014-06-18 MX MX2015017536A patent/MX2015017536A/es unknown
- 2014-06-18 EP EP14732980.9A patent/EP3010926B1/en active Active
- 2014-06-18 BR BR112015029521A patent/BR112015029521A2/pt not_active IP Right Cessation
- 2014-06-18 CN CN201480035390.4A patent/CN105324386B/zh active Active
- 2014-06-18 WO PCT/IB2014/062375 patent/WO2014203185A1/en active Application Filing
- 2014-06-18 KR KR1020167001145A patent/KR20160021243A/ko not_active Application Discontinuation
- 2014-06-18 US US14/895,523 patent/US20160130280A1/en not_active Abandoned
- 2014-06-18 CA CA2911104A patent/CA2911104A1/en not_active Abandoned
- 2014-06-18 JP JP2016520793A patent/JP6574173B2/ja active Active
- 2014-06-18 AU AU2014282831A patent/AU2014282831B2/en not_active Ceased
- 2014-06-18 RU RU2015156316A patent/RU2691728C2/ru active
-
2015
- 2015-11-02 IL IL242413A patent/IL242413B/en active IP Right Grant
-
2016
- 2016-06-30 HK HK16107634.9A patent/HK1219727A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2014282831B2 (en) | 2016-12-01 |
| IL242413B (en) | 2018-04-30 |
| CA2911104A1 (en) | 2014-12-24 |
| BR112015029521A2 (pt) | 2017-07-25 |
| US20160130280A1 (en) | 2016-05-12 |
| RU2015156316A (ru) | 2017-07-25 |
| CN105324386A (zh) | 2016-02-10 |
| CN105324386B (zh) | 2019-02-19 |
| EP3010926A1 (en) | 2016-04-27 |
| EP3010926B1 (en) | 2019-11-20 |
| CN109651396A (zh) | 2019-04-19 |
| RU2691728C2 (ru) | 2019-06-18 |
| JP6574173B2 (ja) | 2019-09-11 |
| HK1219727A1 (zh) | 2017-04-13 |
| WO2014203185A1 (en) | 2014-12-24 |
| JP2016523246A (ja) | 2016-08-08 |
| CN109651396B (zh) | 2021-09-14 |
| KR20160021243A (ko) | 2016-02-24 |
| AU2014282831A1 (en) | 2015-11-12 |
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