JP6574173B2 - 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 - Google Patents

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 Download PDF

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Publication number
JP6574173B2
JP6574173B2 JP2016520793A JP2016520793A JP6574173B2 JP 6574173 B2 JP6574173 B2 JP 6574173B2 JP 2016520793 A JP2016520793 A JP 2016520793A JP 2016520793 A JP2016520793 A JP 2016520793A JP 6574173 B2 JP6574173 B2 JP 6574173B2
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Prior art keywords
alkyl
base
sulfonate
everolimus
protecting group
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Japanese (ja)
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JP2016523246A (ja
JP2016523246A5 (enExample
Inventor
アシモグル，ムラート
ヴィーチ，ジェマ
Original Assignee
ノバルティス アーゲー
ノバルティス アーゲー
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
JP2016520793A 2013-06-20 2014-06-18 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 Expired - Fee Related JP6574173B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361837224P 2013-06-20 2013-06-20
US61/837,224 2013-06-20
PCT/IB2014/062375 WO2014203185A1 (en) 2013-06-20 2014-06-18 Alkylation with an alkyl fluoroalkyl sulfonate

Publications (3)

Publication Number Publication Date
JP2016523246A JP2016523246A (ja) 2016-08-08
JP2016523246A5 JP2016523246A5 (enExample) 2017-08-03
JP6574173B2 true JP6574173B2 (ja) 2019-09-11

Family

ID=51014598

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016520793A Expired - Fee Related JP6574173B2 (ja) 2013-06-20 2014-06-18 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

Country Status (13)

Country Link
US (1) US20160130280A1 (enExample)
EP (1) EP3010926B1 (enExample)
JP (1) JP6574173B2 (enExample)
KR (1) KR20160021243A (enExample)
CN (2) CN105324386B (enExample)
AU (1) AU2014282831B2 (enExample)
BR (1) BR112015029521A2 (enExample)
CA (1) CA2911104A1 (enExample)
HK (1) HK1219727A1 (enExample)
IL (1) IL242413B (enExample)
MX (1) MX2015017536A (enExample)
RU (1) RU2691728C2 (enExample)
WO (1) WO2014203185A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
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
CN116082363B (zh) * 2023-02-16 2025-11-21 西安交通大学 一种雷帕霉素40-位羟基的烷基化合成方法

Family Cites Families (10)

* 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
DE69624921T2 (de) * 1995-06-09 2003-09-11 Novartis Ag, Basel Rapamycinderivate
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
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
EP1571151B1 (en) 2004-03-01 2008-12-24 Terumo Kabushiki Kaisha Process for production of O-alkylated rapamycin derivatives
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
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

Also Published As

Publication number Publication date
CN109651396A (zh) 2019-04-19
KR20160021243A (ko) 2016-02-24
CN105324386B (zh) 2019-02-19
WO2014203185A1 (en) 2014-12-24
CN109651396B (zh) 2021-09-14
IL242413B (en) 2018-04-30
HK1219727A1 (zh) 2017-04-13
EP3010926B1 (en) 2019-11-20
US20160130280A1 (en) 2016-05-12
BR112015029521A2 (pt) 2017-07-25
AU2014282831B2 (en) 2016-12-01
EP3010926A1 (en) 2016-04-27
CA2911104A1 (en) 2014-12-24
MX2015017536A (es) 2016-04-26
CN105324386A (zh) 2016-02-10
RU2015156316A (ru) 2017-07-25
RU2691728C2 (ru) 2019-06-18
AU2014282831A1 (en) 2015-11-12
JP2016523246A (ja) 2016-08-08

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