UY36746A - Método para la síntesis de derivados de rapamicina - Google Patents
Método para la síntesis de derivados de rapamicinaInfo
- Publication number
- UY36746A UY36746A UY0001036746A UY36746A UY36746A UY 36746 A UY36746 A UY 36746A UY 0001036746 A UY0001036746 A UY 0001036746A UY 36746 A UY36746 A UY 36746A UY 36746 A UY36746 A UY 36746A
- Authority
- UY
- Uruguay
- Prior art keywords
- triflate
- synthesis
- rapamycin
- rapamycin derivatives
- tri
- Prior art date
Links
Classifications
-
- 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
-
- 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
- C07D498/16—Peri-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención describe un método para producir un derivado de rapamicina de fórmula (I), el método incluye preparar un triflato de 2-(tri-sustituido silil) oxietilo por la reacción del óxido de etileno y un triflato de sililo tri-sustituido, la reacción del triflato 2-(trisustituido sililo)oxietilo con rapamicina en presencia de un exceso molar de base orgánica, y la desprotección para obtener el derivado rapamicina del compuesto (I).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP15173283.1A EP3109250A1 (en) | 2015-06-23 | 2015-06-23 | Method for the synthesis of rapamycin derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
UY36746A true UY36746A (es) | 2016-12-30 |
Family
ID=53488213
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
UY0001036746A UY36746A (es) | 2015-06-23 | 2016-06-22 | Método para la síntesis de derivados de rapamicina |
Country Status (16)
Country | Link |
---|---|
US (1) | US10308665B2 (es) |
EP (2) | EP3109250A1 (es) |
JP (1) | JP6745823B2 (es) |
KR (1) | KR102621941B1 (es) |
CN (1) | CN107735398B (es) |
AR (1) | AR105091A1 (es) |
AU (1) | AU2016282816A1 (es) |
ES (1) | ES2741013T3 (es) |
HU (1) | HUE045651T2 (es) |
MX (1) | MX2017017022A (es) |
PL (1) | PL3313853T3 (es) |
RU (1) | RU2718058C2 (es) |
SI (1) | SI3313853T1 (es) |
TW (1) | TWI646100B (es) |
UY (1) | UY36746A (es) |
WO (1) | WO2016207205A1 (es) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR102641816B1 (ko) | 2016-07-19 | 2024-02-29 | 삼성디스플레이 주식회사 | 디스플레이 장치 |
CN109206441B (zh) * | 2017-06-30 | 2022-05-20 | 正大天晴药业集团股份有限公司 | 一种依维莫司的纯化方法 |
CN109776571B (zh) * | 2019-01-31 | 2021-06-11 | 哈药慈航制药股份有限公司 | 一种雷帕霉素类似物及其制备方法和应用 |
RU2716714C1 (ru) * | 2019-08-26 | 2020-03-16 | Закрытое Акционерное Общество "Биокад" | Новый способ получения эверолимуса |
CN113735880B (zh) * | 2020-05-29 | 2023-12-22 | 鲁南制药集团股份有限公司 | 一种依维莫司的制备方法及其中间体 |
CN115028658A (zh) * | 2022-07-06 | 2022-09-09 | 国药集团川抗制药有限公司 | 雷帕霉素硅醇酯及其制备方法和应用 |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
GB0601406D0 (en) * | 2006-01-24 | 2006-03-08 | Novartis Ag | Organic Compounds |
GB0609962D0 (en) | 2006-05-19 | 2006-06-28 | Biotica Tech Ltd | Novel compounds |
CN102127092B (zh) * | 2010-01-18 | 2013-04-17 | 东南大学 | 依维莫斯的制备 |
US9079921B2 (en) | 2010-11-19 | 2015-07-14 | Biocon Limited | Processes for preparation of Everolimus and intermediates thereof |
EP2670758B1 (en) | 2011-02-04 | 2022-09-28 | Synthon BV | Process for making trisubstituted silyloxyethyl triflates |
CN102268015B (zh) | 2011-08-30 | 2013-08-28 | 成都摩尔生物医药有限公司 | 一种依维莫司的合成方法 |
CN102786534A (zh) | 2012-05-25 | 2012-11-21 | 上海现代制药股份有限公司 | 一种依维莫司的制备方法 |
JP2016500112A (ja) * | 2012-11-30 | 2016-01-07 | ハンジョウ ジロックス ファーマ カンパニー リミテッドHangzhou Zylox Pharma Co.,Ltd. | ラパマイシン類似体及びその製作方法 |
CA2911104A1 (en) | 2013-06-20 | 2014-12-24 | Novartis Ag | Alkylation with an alkyl fluoroalkyl sulfonate |
CN103848849B (zh) * | 2014-03-24 | 2016-02-24 | 上海医药工业研究院 | 依维莫司的制备工艺 |
CN104478898A (zh) | 2014-11-18 | 2015-04-01 | 连云港恒运医药科技有限公司 | 依维莫司及其中间体的制备方法 |
-
2015
- 2015-06-23 EP EP15173283.1A patent/EP3109250A1/en not_active Withdrawn
-
2016
- 2016-06-22 RU RU2017144050A patent/RU2718058C2/ru active
- 2016-06-22 MX MX2017017022A patent/MX2017017022A/es unknown
- 2016-06-22 KR KR1020187001488A patent/KR102621941B1/ko active IP Right Grant
- 2016-06-22 TW TW105119625A patent/TWI646100B/zh active
- 2016-06-22 HU HUE16731862A patent/HUE045651T2/hu unknown
- 2016-06-22 EP EP16731862.5A patent/EP3313853B1/en active Active
- 2016-06-22 US US15/737,861 patent/US10308665B2/en active Active
- 2016-06-22 CN CN201680036479.1A patent/CN107735398B/zh active Active
- 2016-06-22 UY UY0001036746A patent/UY36746A/es not_active Application Discontinuation
- 2016-06-22 AR ARP160101863A patent/AR105091A1/es unknown
- 2016-06-22 WO PCT/EP2016/064389 patent/WO2016207205A1/en active Application Filing
- 2016-06-22 ES ES16731862T patent/ES2741013T3/es active Active
- 2016-06-22 JP JP2017566621A patent/JP6745823B2/ja active Active
- 2016-06-22 SI SI201630337T patent/SI3313853T1/sl unknown
- 2016-06-22 PL PL16731862T patent/PL3313853T3/pl unknown
- 2016-06-22 AU AU2016282816A patent/AU2016282816A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
RU2017144050A (ru) | 2019-07-23 |
SI3313853T1 (sl) | 2019-10-30 |
US20190010168A1 (en) | 2019-01-10 |
PL3313853T3 (pl) | 2020-01-31 |
RU2718058C2 (ru) | 2020-03-30 |
KR20180015257A (ko) | 2018-02-12 |
CN107735398A (zh) | 2018-02-23 |
HUE045651T2 (hu) | 2020-01-28 |
EP3109250A1 (en) | 2016-12-28 |
JP2018518504A (ja) | 2018-07-12 |
MX2017017022A (es) | 2018-08-15 |
JP6745823B2 (ja) | 2020-08-26 |
RU2017144050A3 (es) | 2019-11-11 |
EP3313853A1 (en) | 2018-05-02 |
ES2741013T3 (es) | 2020-02-07 |
WO2016207205A1 (en) | 2016-12-29 |
TW201713669A (zh) | 2017-04-16 |
US10308665B2 (en) | 2019-06-04 |
EP3313853B1 (en) | 2019-05-08 |
KR102621941B1 (ko) | 2024-01-05 |
TWI646100B (zh) | 2019-01-01 |
AU2016282816A1 (en) | 2018-01-04 |
CN107735398B (zh) | 2020-07-31 |
AR105091A1 (es) | 2017-09-06 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
109 | Application deemed to be withdrawn |
Effective date: 20221129 |