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PE20180504A1 - PROCESOS E INTERMEDIARIOS PARA LA PREPARACION DE {1-(ETILSULFONIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO - Google Patents

PROCESOS E INTERMEDIARIOS PARA LA PREPARACION DE {1-(ETILSULFONIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO

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Publication number
PE20180504A1
PE20180504A1 PE2017002470A PE2017002470A PE20180504A1 PE 20180504 A1 PE20180504 A1 PE 20180504A1 PE 2017002470 A PE2017002470 A PE 2017002470A PE 2017002470 A PE2017002470 A PE 2017002470A PE 20180504 A1 PE20180504 A1 PE 20180504A1
Authority
PE
Peru
Prior art keywords
azetidin
acetonitrile
ethylsulfonyl
pyrimidin
ethylsulfonylazetidin
Prior art date
Application number
PE2017002470A
Other languages
English (en)
Inventor
Michael E Kopach
Joseph R Martinelli
David Lee Varie
Thomas Michael Wilson
Michael Edward Kobierski
Original Assignee
Lilly Co Eli
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=56204068&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20180504(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20180504A1 publication Critical patent/PE20180504A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se refiere a un proceso de preparacion de {1-(etilsulfonil)-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrilo, de formula I, el cual comprende las etapas de: acoplar clorhdirato de azetidin-3-ol con cloruro de etansulfonilo para dar 1-etilsulfonilazetidin-3-ol; oxidacion aerobica de 1-etilsulfonilazetidin-3-ol a 1-etilsulfonilazetidin-3-ona en presencia de un reactivo de nitroxilo, un agente oxidante, y un acido; reaccion de 1-etilsulfonilazetidin-3-ona con un reactivo de fosfonato en presencia de una base; opcionalmente cristalizar [1-(etilsulfonil)azetidin-3-iliden]acetonitrilo; opcionalmente proteger 4-(4,4,5,5,-tetrametil-1,3,2-dioxaborolan-2-il)-1H-pirazol con un grupo protector de N; acoplar [1-(etilsulfonil)azetidin-3-iliden]acetonitrilo con 4-(4,4,5,5,-tetrametil-1,3,2-dioxaborolan-2-il)-1H-pirazol; opcionalmente cristalizar {1-(etilsulfonil)-3-[4,4,5,5,-tetrametil-1,3,2-dioxaborolan-2-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrilo; opcionalmente proteger 4-cloro-7H-pirrolo[2,3-d]pirimidina; acoplar {1-(etilsulfonil)-3-[4-(4,4,5,5,-tetrametil-1,3,2-dioxaborolan-2-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrilo y 4-cloro-7H-pirrolo[2,3-d]pirimidina usando un catalizador de Pd en presencia de una base para obtener {1-(etilsulfonil)-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrilo.
PE2017002470A 2015-06-19 2016-06-16 PROCESOS E INTERMEDIARIOS PARA LA PREPARACION DE {1-(ETILSULFONIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO PE20180504A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562182040P 2015-06-19 2015-06-19

Publications (1)

Publication Number Publication Date
PE20180504A1 true PE20180504A1 (es) 2018-03-09

Family

ID=56204068

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017002470A PE20180504A1 (es) 2015-06-19 2016-06-16 PROCESOS E INTERMEDIARIOS PARA LA PREPARACION DE {1-(ETILSULFONIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO

Country Status (26)

Country Link
US (2) US20180134713A1 (es)
EP (1) EP3310781A1 (es)
JP (1) JP2018519280A (es)
KR (1) KR20180008637A (es)
CN (1) CN107660206A (es)
AR (1) AR104918A1 (es)
AU (1) AU2016280815A1 (es)
BR (1) BR112017024613A2 (es)
CA (1) CA2984627A1 (es)
CL (1) CL2017003112A1 (es)
CO (1) CO2017013226A2 (es)
CR (1) CR20170533A (es)
DO (1) DOP2017000300A (es)
EA (1) EA201792308A1 (es)
EC (1) ECSP17083426A (es)
HK (1) HK1248699A1 (es)
IL (1) IL255386A0 (es)
MA (1) MA45901A (es)
MX (1) MX2017015837A (es)
NZ (1) NZ736999A (es)
PE (1) PE20180504A1 (es)
PH (1) PH12017502360A1 (es)
SV (1) SV2017005586A (es)
TN (1) TN2017000530A1 (es)
TW (1) TWI622591B (es)
WO (1) WO2016205487A1 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108341818A (zh) * 2017-01-21 2018-07-31 南京华威医药科技开发有限公司 巴瑞克替尼及其磷酸盐的新晶型及其制备方法
CA3055233C (en) 2017-01-23 2022-08-09 Shanghai Longwood Biopharmaceuticals Co., Ltd. Jak kinase inhibitor and preparation method and use thereof
CN106946917B (zh) * 2017-03-20 2019-06-11 杭州科巢生物科技有限公司 一种jak抑制剂巴瑞替尼及其中间体的新合成方法
CN107739328B (zh) * 2017-11-22 2020-03-20 海化生命(厦门)科技有限公司 用于合成巴瑞替尼的关键中间体1的制备方法
CN108129482A (zh) * 2017-12-13 2018-06-08 江苏中邦制药有限公司 一种巴瑞替尼的制备方法
US10766900B2 (en) 2017-12-29 2020-09-08 Formosa Laboratories, Inc. Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
WO2020072870A1 (en) 2018-10-05 2020-04-09 Johnson Matthey Public Limited Company Co-crystal forms of baricitinib
TW202033198A (zh) 2018-10-17 2020-09-16 美商美國禮來大藥廠 以巴瑞克替尼(baricitinib)治療原發性膽汁性膽管炎及原發性硬化性膽管炎
KR20250057082A (ko) 2019-04-24 2025-04-28 엘랑코 유에스 인코포레이티드 7h-피롤로[2,3-d]피리미딘 jak-억제제
CN117729924A (zh) 2021-07-30 2024-03-19 伊莱利利公司 用巴瑞克替尼治疗手部湿疹
CN117720543A (zh) * 2023-12-13 2024-03-19 东北林业大学 一种巴瑞替尼的制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5821374A (en) * 1995-11-21 1998-10-13 Hoffmann-La Roche Inc. Process for the oxidation of alcohols
UA101493C2 (ru) * 2008-03-11 2013-04-10 Инсайт Корпорейшн Производные азетидина и циклобутана как ингибиторы jak
CA2796388A1 (en) * 2010-04-14 2011-10-20 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
CN102557901B (zh) * 2010-12-15 2014-06-11 上海医药工业研究院 6-氯己醛的制备方法
DK2964650T3 (en) * 2013-03-06 2019-02-11 Incyte Holdings Corp PROCEDURES AND INTERMEDIATES FOR THE MANUFACTURE OF A JAK INHIBITOR
CN105541891B (zh) * 2016-02-04 2017-11-28 东南大学 巴瑞替尼的中间体及其制备方法及由该中间体制备巴瑞替尼的方法

Also Published As

Publication number Publication date
US20190062337A1 (en) 2019-02-28
EP3310781A1 (en) 2018-04-25
WO2016205487A1 (en) 2016-12-22
TWI622591B (zh) 2018-05-01
IL255386A0 (en) 2017-12-31
MX2017015837A (es) 2018-04-10
AR104918A1 (es) 2017-08-23
EA201792308A1 (ru) 2018-05-31
DOP2017000300A (es) 2018-01-31
SV2017005586A (es) 2018-04-24
JP2018519280A (ja) 2018-07-19
HK1248699A1 (zh) 2018-10-19
MA45901A (fr) 2019-06-19
CR20170533A (es) 2018-01-25
AU2016280815A1 (en) 2017-11-23
TW201712015A (zh) 2017-04-01
CN107660206A (zh) 2018-02-02
US20180134713A1 (en) 2018-05-17
NZ736999A (en) 2019-05-31
ECSP17083426A (es) 2018-02-28
PH12017502360A1 (en) 2018-06-25
CL2017003112A1 (es) 2018-06-01
KR20180008637A (ko) 2018-01-24
CO2017013226A2 (es) 2018-03-28
TN2017000530A1 (en) 2019-04-12
BR112017024613A2 (pt) 2018-07-31
CA2984627A1 (en) 2016-12-22

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