CN105324386B - 氟代烷基磺酸烷基酯的烷基化 - Google Patents

氟代烷基磺酸烷基酯的烷基化 Download PDF

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Publication number
CN105324386B
CN105324386B CN201480035390.4A CN201480035390A CN105324386B CN 105324386 B CN105324386 B CN 105324386B CN 201480035390 A CN201480035390 A CN 201480035390A CN 105324386 B CN105324386 B CN 105324386B
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CN105324386A (zh
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M·埃斯莫格鲁
G·维奇
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Novartis AG
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Novartis AG
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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)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Transplantation (AREA)
  • Epidemiology (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)
CN201480035390.4A 2013-06-20 2014-06-18 氟代烷基磺酸烷基酯的烷基化 Active CN105324386B (zh)

Priority Applications (1)

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CN201910054592.8A CN109651396B (zh) 2013-06-20 2014-06-18 氟代烷基磺酸烷基酯的烷基化

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

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CN201910054592.8A Division CN109651396B (zh) 2013-06-20 2014-06-18 氟代烷基磺酸烷基酯的烷基化

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CN105324386A CN105324386A (zh) 2016-02-10
CN105324386B true CN105324386B (zh) 2019-02-19

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CN201910054592.8A Active CN109651396B (zh) 2013-06-20 2014-06-18 氟代烷基磺酸烷基酯的烷基化

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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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090292118A1 (en) * 2008-05-26 2009-11-26 Kwang-Chung Lee Process for making Biolimus A9
CN102127092A (zh) * 2010-01-18 2011-07-20 东南大学 依维莫斯的制备
WO2012103959A1 (en) * 2011-02-04 2012-08-09 Synthon Bv Process for making everolimus

Family Cites Families (7)

* 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
KR100400620B1 (ko) * 1995-06-09 2004-02-18 노파르티스 아게 라파마이신유도체
WO1998009970A2 (en) * 1996-09-09 1998-03-12 American Home Products Corporation Alkylated rapamycin derivatives
ES2315745T3 (es) 2004-03-01 2009-04-01 Terumo Kabushiki Kaisha Procedimiento para la fabricacion de derivados o-alquilados de rapamicina.
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
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.
WO2012066502A1 (en) 2010-11-19 2012-05-24 Biocon Limited Processes for preparation of everolimus and intermediates thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090292118A1 (en) * 2008-05-26 2009-11-26 Kwang-Chung Lee Process for making Biolimus A9
CN102127092A (zh) * 2010-01-18 2011-07-20 东南大学 依维莫斯的制备
WO2012103959A1 (en) * 2011-02-04 2012-08-09 Synthon Bv Process for making everolimus

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
a large-scale preparation of (3S,4S)-3-(tert-butoxycarbonyl) amino-4-methylpyrrolidine and its analogs from L-aspartic acid;Yoshida T et al.;《chemical and pharmaceutical bulletin》;19960531;第44卷(第5期);第1128-1131页，第1130页倒数第1段至第1131页第2段 *
Concise Synthesis of the Calicheamicin Oligosaccharide Using the Sulfoxide Glycosylation Method;Soong-Hoon Kim et al.;《J. Am. Chem. SOC》;19941231;第116卷(第5期);第1766-1775页，第1770页左栏倒数第2段 *

Also Published As

Publication number Publication date
HK1219727A1 (zh) 2017-04-13
RU2691728C2 (ru) 2019-06-18
KR20160021243A (ko) 2016-02-24
AU2014282831B2 (en) 2016-12-01
CA2911104A1 (en) 2014-12-24
IL242413B (en) 2018-04-30
CN105324386A (zh) 2016-02-10
WO2014203185A1 (en) 2014-12-24
RU2015156316A (ru) 2017-07-25
EP3010926A1 (en) 2016-04-27
CN109651396A (zh) 2019-04-19
MX2015017536A (es) 2016-04-26
BR112015029521A2 (pt) 2017-07-25
CN109651396B (zh) 2021-09-14
JP2016523246A (ja) 2016-08-08
AU2014282831A1 (en) 2015-11-12
US20160130280A1 (en) 2016-05-12
EP3010926B1 (en) 2019-11-20
JP6574173B2 (ja) 2019-09-11

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