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 (11)

* 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
LT3898637T (lt) 2018-12-18 2025-03-10 Novartis Ag Rapamicino dariniai
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
KR20260115158A (ko) 2019-03-26 2026-07-23 노파르티스 아게 이소티아졸리딘 1,1-디옥시드 및 1,4-부탄 술톤 함유 라파마이신 유도체 및 이의 용도
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
CN114671891A (zh) * 2020-12-24 2022-06-28 鲁南制药集团股份有限公司 一种依维莫司乙基化杂质的制备方法
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
GB202415232D0 (en) 2024-10-16 2024-11-27 Nacamed As Composition

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
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
SG11201404432QA (en) * 2012-11-30 2014-10-30 Hangzhou Zylox Pharma Co Ltd Rafamycin analogs and methods for making same
JP6574173B2 (ja) 2013-06-20 2019-09-11 ノバルティス アーゲー アルキルフルオロアルキルスルホネートによるアルキル化
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
TW201713669A (zh) 2017-04-16
ES2741013T3 (es) 2020-02-07
EP3109250A1 (en) 2016-12-28
AU2016282816A1 (en) 2018-01-04
EP3313853A1 (en) 2018-05-02
EP3313853B1 (en) 2019-05-08
RU2718058C2 (ru) 2020-03-30
HUE045651T2 (hu) 2020-01-28
JP6745823B2 (ja) 2020-08-26
TWI646100B (zh) 2019-01-01
KR20180015257A (ko) 2018-02-12
CN107735398A (zh) 2018-02-23
KR102621941B1 (ko) 2024-01-05
SI3313853T1 (sl) 2019-10-30
US20190010168A1 (en) 2019-01-10
RU2017144050A (ru) 2019-07-23
JP2018518504A (ja) 2018-07-12
MX2017017022A (es) 2018-08-15
WO2016207205A1 (en) 2016-12-29
US10308665B2 (en) 2019-06-04
CN107735398B (zh) 2020-07-31
PL3313853T3 (pl) 2020-01-31
AR105091A1 (es) 2017-09-06
RU2017144050A3 (es) 2019-11-11

Similar Documents

Publication Publication Date Title
AR132627A2 (es) Procesos para preparar compuestos intermediarios de utilidad para sintetizar compuestos de carbamoilpiridona policíclicos
MX2017017022A (es) Metodo para la sintesis de derivados de rapamicina.
NZ726356A (en) Processes for preparing antiviral compounds
CO2017013229A2 (es) Agonistas de receptor de apelina (apj) de 4-hidroxi-3-(heteroaril)piridin-2-ona como para uso en el tratamiento de trastornos cardiovasculares
BR112014019909A8 (pt) Processo para produção de compostos úteis como antagonistas do receptor de orexina-2
BR112014030365A2 (pt) síntese de composto antiviral
CU24408B1 (es) Compuestos de dihidroisoquinolinona sustituida
CL2018002094A1 (es) Un proceso para preparar compuesto de pirrolo[3,2–d]pirimidina y su intermediario
AR116790A1 (es) PROCEDIMIENTO PARA LA PREPARACIÓN DE 3a-HIDROXI-5a-PREGNAN-20-ONA (BREXANOLONA)
EA201591815A1 (ru) Бицикло [2.2.2] кислоты - модуляторы gpr120
EA201590949A1 (ru) Дигидропиразольные модуляторы gpr40
CY1120763T1 (el) Νεες ενωσεις σουλφονυλαμινοβενζαμιδιου
CR20170134A (es) Método para preparar 2´-o-fucosil-lactosa
MX369857B (es) Pirazinas moduladoras de receptor 6 acoplado a la proteina g (gpr6).
BR112017019850A2 (pt) ?processo melhorado para a preparação de apremilast?
CL2018002756A1 (es) Un proceso mejorado para la preparación de tartrato de butorfanol.
CY1121116T1 (el) Νεα μεθοδος για την συνθεση αγομελατινης
NZ720106A (en) A process for the preparation of regadenoson
BR112016022437A2 (pt) Processo para preparação de (2s,5r)-6-(benziloxi)-7-oxo-1,6- diazabiciclo[3,2,1]octano-2-carboxilato de sódio
MX2018003903A (es) Compuesto biciclico y uso del mismo para inhibicion de suv39h2.
BR112016021910A2 (pt) Processo de preparação de 3-(3-(4-(1-aminociclobutil)fenil)-5-fenil-3h-imidazo[4,5-b]piridin-2-il)piridin-2-amina
PH12017501404A1 (en) Diaza-benzofluoranthrene compounds
MX2020009462A (es) Procesos para la preparación de compuestos de pirimidinilciclopentano.
MX2018008718A (es) Metodo para la preparacion de 2-aril-etanoles sustituido.
CU20190035A7 (es) Derivados sustituidos de 6-(1h-pirazol-1-il)pirimidin-4-amina

Legal Events

Date Code Title Description
109 Application deemed to be withdrawn

Effective date: 20221129