AR110356A1 - Proceso para la preparación de 2-(3-(fluormetil)azetidin-1-il)etan-1-ol - Google Patents

Proceso para la preparación de 2-(3-(fluormetil)azetidin-1-il)etan-1-ol

Info

Publication number
AR110356A1
AR110356A1 ARP170103481A ARP170103481A AR110356A1 AR 110356 A1 AR110356 A1 AR 110356A1 AR P170103481 A ARP170103481 A AR P170103481A AR P170103481 A ARP170103481 A AR P170103481A AR 110356 A1 AR110356 A1 AR 110356A1
Authority
AR
Argentina
Prior art keywords
formula
azetidin
fluoromethyl
tetrahydro
oxy
Prior art date
Application number
ARP170103481A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR110356A1 publication Critical patent/AR110356A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Se describen métodos de preparación de 2-(3-(fluormetil)azetidin-1-il)etan-1-ol de fórmula (1), un producto intermedio útil para la síntesis de compuestos modulares del receptor de estrógeno. Reivindicación 1: Un proceso para la preparación de 2-(3-(fluormetil)azetidin-1-il)etan-1-ol de fórmula (1) que comprende hacer reaccionar 3-(fluormetil)azetidina de fórmula (2), glioxalato de etilo, y un primer agente reductor de hidruro para formar 2-(3-(fluormetil)azetidin-1-il)acetato de etilo de fórmula (3); y hacer reaccionar el compuesto de fórmula (3) con un segundo agente reductor de hidruro para formar el compuesto de fórmula (1). Reivindicación 17: El proceso de la reivindicación 1, que además comprende hacer reaccionar el compuesto de fórmula (1) y 2-(4-yodofenil)-4-metil-6-((tetrahidro-2H-piran-2-il)oxi)-3-(3-((tetrahidro-2H-piran-2-il)oxi)-2H-cromeno de fórmula (4) para formar 3-(fluormetil)-1-(2-(4-(4-metil-6-((tetrahidro-2H-piran-2-il)oxi)-3-(3-((tetrahidro-2H-piran-2-il)oxi)fenil)-2H-cromen-2-il)fenoxi)etil)azetidina de fórmula (5). Reivindicación 18: El proceso de la reivindicación 17, que además comprende hacer reaccionar el compuesto de fórmula (5) con ácido acético acuoso para formar 2-(4-(2-(3-(fluormetil)azetidin-1-ii)etoxi)fenil)-3-(3-hidroxifenil)-4-metil-2H-cromen-6-ol de fórmula (6).
ARP170103481A 2016-12-12 2017-12-13 Proceso para la preparación de 2-(3-(fluormetil)azetidin-1-il)etan-1-ol AR110356A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662432837P 2016-12-12 2016-12-12

Publications (1)

Publication Number Publication Date
AR110356A1 true AR110356A1 (es) 2019-03-20

Family

ID=60935792

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170103481A AR110356A1 (es) 2016-12-12 2017-12-13 Proceso para la preparación de 2-(3-(fluormetil)azetidin-1-il)etan-1-ol

Country Status (2)

Country Link
AR (1) AR110356A1 (es)
WO (1) WO2018108954A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI702219B (zh) 2018-07-12 2020-08-21 美商美國禮來大藥廠 選擇性雌激素受體降解劑
CN114933551B (zh) * 2022-06-28 2023-06-30 吉尔多肽生物制药(大连市)有限公司 一种手性Fmoc-3-氨基-2-(叔丁氧基甲基)丙酸的合成方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008514595A (ja) * 2004-09-24 2008-05-08 アストラゼネカ・アクチエボラーグ 化合物、それを含有する組成物、その製造及びその使用ii
WO2007023768A1 (ja) * 2005-08-24 2007-03-01 Eisai R & D Management Co., Ltd. 新規ピリジン誘導体およびピリミジン誘導体(3)
WO2013090829A1 (en) 2011-12-14 2013-06-20 Aragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
MX2015016171A (es) 2013-06-19 2016-08-08 Seragon Pharmaceuticals Inc Moduladores del receptor de estrogeno de azetidina y usos de los mismos.
SG11201509508YA (en) 2013-06-19 2015-12-30 Seragon Pharmaceuticals Inc Estrogen receptor modulator and uses thereof
MA53837A (fr) 2014-12-18 2021-11-10 Hoffmann La Roche Tetrahydro-pyrido[3,4-b]indoles modulateurs des récepteurs des oestrogènes et leurs utilisations
US20160175284A1 (en) 2014-12-18 2016-06-23 Genentech, Inc. Estrogen receptor modulators and uses thereof
EP3233828B1 (en) 2014-12-18 2020-03-04 F. Hoffmann-La Roche AG Estrogen receptor modulators and uses thereof

Also Published As

Publication number Publication date
WO2018108954A1 (en) 2018-06-21

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