AR105091A1 - Procedimiento para la síntesis de derivados de rapamicina - Google Patents

Procedimiento para la síntesis de derivados de rapamicina

Info

Publication number
AR105091A1
AR105091A1 ARP160101863A ARP160101863A AR105091A1 AR 105091 A1 AR105091 A1 AR 105091A1 AR P160101863 A ARP160101863 A AR P160101863A AR P160101863 A ARP160101863 A AR P160101863A AR 105091 A1 AR105091 A1 AR 105091A1
Authority
AR
Argentina
Prior art keywords
formula
triflate
trisubstituted
rapamycin
rapamycin derivative
Prior art date
Application number
ARP160101863A
Other languages
English (en)
Inventor
Sypchenko Volodymyr
Matviienko Iaroslav
Schickaneder Christian
Zabudkin Oleksandr
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 AR105091A1 publication Critical patent/AR105091A1/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 se refiere a un procedimiento para la producción de un derivado de rapamicina de fórmula (1), comprendiendo el procedimiento la preparación de un triflato de 2-(sililo trisustituido)oxietilo mediante la reacción de óxido de etileno y un triflato de sililo trisustituido, la reacción del triflato de 2-(sililo trisustituido)oxietilo resultante con rapamicina en presencia de un exceso molar de base orgánica, y la desprotección para obtener el derivado de rapamicina del compuesto de fórmula (1). Reivindicación 1: Procedimiento para la producción de un derivado de rapamicina de fórmula (1), caracterizado porque comprende: (a) preparar un triflato de 2-(sililo trisustituido)oxietilo de fórmula (3) mediante la reacción de óxido de etileno y un triflato de sililo trisustituido de fórmula (2) en el que R¹, R², y R³ se seleccionaron en forma independiente del grupo que consiste de alquilo C₁₋₁₂ y arilo C₁₋₁₂; (b) hacer reaccionar el triflato de 2-(sililo trisustituido)oxietilo de fórmula (3) obtenido en el paso (a) con rapamicina en presencia de un exceso molar de base orgánica para obtener un derivado de rapamicina protegido de fórmula (4); y (c) desproteger el derivado de rapamicina protegido de fórmula (4) para obtener el derivado de rapamicina si es la fórmula (1).
ARP160101863A 2015-06-23 2016-06-22 Procedimiento para la síntesis de derivados de rapamicina AR105091A1 (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
AR105091A1 true AR105091A1 (es) 2017-09-06

Family

ID=53488213

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160101863A AR105091A1 (es) 2015-06-23 2016-06-22 Procedimiento 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 (7)

* 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
UY37900A (es) 2017-09-26 2019-04-30 Novartis Ag Nuevos derivados de rapamicina
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
ES2753529T3 (es) 2010-11-19 2020-04-13 Biocon Ltd Procesos para la preparación de everolimús y productos intermedios del mismo
WO2012103960A1 (en) * 2011-02-04 2012-08-09 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
CN104854112A (zh) * 2012-11-30 2015-08-19 杭州归创生物医药有限公司 雷帕霉素类似物及其制备方法
BR112015029521A2 (pt) 2013-06-20 2017-07-25 Novartis Ag alquilação com um sulfonato de alquil fluoroalquila
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
JP2018518504A (ja) 2018-07-12
US20190010168A1 (en) 2019-01-10
KR102621941B1 (ko) 2024-01-05
RU2718058C2 (ru) 2020-03-30
UY36746A (es) 2016-12-30
TW201713669A (zh) 2017-04-16
US10308665B2 (en) 2019-06-04
ES2741013T3 (es) 2020-02-07
RU2017144050A3 (es) 2019-11-11
HUE045651T2 (hu) 2020-01-28
EP3313853B1 (en) 2019-05-08
RU2017144050A (ru) 2019-07-23
CN107735398B (zh) 2020-07-31
KR20180015257A (ko) 2018-02-12
PL3313853T3 (pl) 2020-01-31
EP3109250A1 (en) 2016-12-28
JP6745823B2 (ja) 2020-08-26
EP3313853A1 (en) 2018-05-02
MX2017017022A (es) 2018-08-15
CN107735398A (zh) 2018-02-23
SI3313853T1 (sl) 2019-10-30
TWI646100B (zh) 2019-01-01
AU2016282816A1 (en) 2018-01-04
WO2016207205A1 (en) 2016-12-29

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