UY36746A - Método para la síntesis de derivados de rapamicina - Google Patents

Método para la síntesis de derivados de rapamicina

Info

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
Application number
UY0001036746A
Other languages
English (en)
Inventor
Schickaneder Christian
Iaroslav Matviienko
Volodymyr Sypchenko
Oleksandr Zabudkin
Original Assignee
Synbias Pharma Ag
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Synbias Pharma Ag filed Critical Synbias Pharma Ag
Publication of UY36746A publication Critical patent/UY36746A/es

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).
UY0001036746A 2015-06-23 2016-06-22 Método para la síntesis de derivados de rapamicina UY36746A (es)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
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
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
KR20150003156A (ko) * 2012-11-30 2015-01-08 항조우 질록스 파마 컴퍼니 리니티드 라파마이신 유사체 및 이의 제조 방법
CN109651396B (zh) 2013-06-20 2021-09-14 诺华股份有限公司 氟代烷基磺酸烷基酯的烷基化
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

Also Published As

Publication number Publication date
AU2016282816A1 (en) 2018-01-04
KR20180015257A (ko) 2018-02-12
KR102621941B1 (ko) 2024-01-05
JP2018518504A (ja) 2018-07-12
HUE045651T2 (hu) 2020-01-28
RU2017144050A (ru) 2019-07-23
EP3313853A1 (en) 2018-05-02
PL3313853T3 (pl) 2020-01-31
ES2741013T3 (es) 2020-02-07
TW201713669A (zh) 2017-04-16
CN107735398A (zh) 2018-02-23
WO2016207205A1 (en) 2016-12-29
CN107735398B (zh) 2020-07-31
AR105091A1 (es) 2017-09-06
MX2017017022A (es) 2018-08-15
EP3313853B1 (en) 2019-05-08
RU2017144050A3 (es) 2019-11-11
EP3109250A1 (en) 2016-12-28
US10308665B2 (en) 2019-06-04
US20190010168A1 (en) 2019-01-10
RU2718058C2 (ru) 2020-03-30
SI3313853T1 (sl) 2019-10-30
JP6745823B2 (ja) 2020-08-26
TWI646100B (zh) 2019-01-01

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Legal Events

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Effective date: 20221129