MX2019006783A - Procedimiento para la preparacion de 4-amino-1-( (1s, 4r, 5s) -2-fluoro-4,5-dihidroxi-3-hidroximetil-ciclopent-2-enil)-1h-pirim idin-2-ona. - Google Patents

Procedimiento para la preparacion de 4-amino-1-( (1s, 4r, 5s) -2-fluoro-4,5-dihidroxi-3-hidroximetil-ciclopent-2-enil)-1h-pirim idin-2-ona.

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Publication number
MX2019006783A
MX2019006783A MX2019006783A MX2019006783A MX2019006783A MX 2019006783 A MX2019006783 A MX 2019006783A MX 2019006783 A MX2019006783 A MX 2019006783A MX 2019006783 A MX2019006783 A MX 2019006783A MX 2019006783 A MX2019006783 A MX 2019006783A
Authority
MX
Mexico
Prior art keywords
cyclopent
pyrimidin
dihydroxy
hydroxymethyl
fluoro
Prior art date
Application number
MX2019006783A
Other languages
English (en)
Inventor
Joong Kim Deog
Yin Haifeng
Falb Eliezer
Andre Pearcey Leigh
cummins Jonathan
Dieterich Petra
Carniaux Jean-Francois
Wang Yi
Chandrakant Purohit Vikrain
Original Assignee
Rexahn Pharmaceuticals Inc
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 Rexahn Pharmaceuticals Inc filed Critical Rexahn Pharmaceuticals Inc
Publication of MX2019006783A publication Critical patent/MX2019006783A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/18Radicals substituted by singly bound oxygen or sulfur atoms
    • C07D317/22Radicals substituted by singly bound oxygen or sulfur atoms etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/26Radicals substituted by doubly bound oxygen or sulfur atoms or by two such atoms singly bound to the same carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1872Preparation; Treatments not provided for in C07F7/20
    • C07F7/188Preparation; Treatments not provided for in C07F7/20 by reactions involving the formation of Si-O linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1872Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Health & Medical Sciences (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Se describen procedimientos para la preparación de 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihidroxi-3-hidroximetil-ciclo pent-2-enil)-1H-pirimidin-2-ona (13, RX-3117) y sus intermediarios.
MX2019006783A 2013-03-15 2015-09-10 Procedimiento para la preparacion de 4-amino-1-( (1s, 4r, 5s) -2-fluoro-4,5-dihidroxi-3-hidroximetil-ciclopent-2-enil)-1h-pirim idin-2-ona. MX2019006783A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361800475P 2013-03-15 2013-03-15

Publications (1)

Publication Number Publication Date
MX2019006783A true MX2019006783A (es) 2019-09-05

Family

ID=50639998

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2015012300A MX368669B (es) 2013-03-15 2014-03-17 Procedimiento para la preparación de 4-amino-1-((1s,4r,5s)-2-fluor o-4,5-dihidroxi-3-hidroximetil-ciclopent-2-enil)-1h-pirimidin-2-o na.
MX2019006783A MX2019006783A (es) 2013-03-15 2015-09-10 Procedimiento para la preparacion de 4-amino-1-( (1s, 4r, 5s) -2-fluoro-4,5-dihidroxi-3-hidroximetil-ciclopent-2-enil)-1h-pirim idin-2-ona.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2015012300A MX368669B (es) 2013-03-15 2014-03-17 Procedimiento para la preparación de 4-amino-1-((1s,4r,5s)-2-fluor o-4,5-dihidroxi-3-hidroximetil-ciclopent-2-enil)-1h-pirimidin-2-o na.

Country Status (11)

Country Link
US (3) US9150520B2 (es)
EP (4) EP3246320B1 (es)
JP (2) JP6334676B2 (es)
KR (1) KR20150130472A (es)
CN (3) CN110483413B (es)
AU (3) AU2014232502B8 (es)
BR (2) BR112015023591B1 (es)
CA (2) CA2904374C (es)
ES (3) ES2678085T3 (es)
MX (2) MX368669B (es)
WO (1) WO2014145807A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110483413B (zh) * 2013-03-15 2023-02-28 百缮药业(苏州)有限公司 用于制备碳环糖衍生物的方法
CN107750160B (zh) 2015-06-09 2021-06-22 百缮药业(苏州)有限公司 氟代环戊烯基胞嘧啶的用途及制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4968690A (en) * 1986-05-27 1990-11-06 United States Government As Represented By The Secretary Of The Dept. Of Health And Human Services 3-deazaneplanocin, intermediates for it, and antiviral composition and method of treatment using it
US4820508A (en) * 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
US4938949A (en) * 1988-09-12 1990-07-03 University Of New York Treatment of damaged bone marrow and dosage units therefor
EP1732902B1 (en) * 2004-04-01 2009-12-30 Rexahn Pharmaceuticals, Inc. Nucleoside derivatives and therapeutic use thereof
CN110483413B (zh) * 2013-03-15 2023-02-28 百缮药业(苏州)有限公司 用于制备碳环糖衍生物的方法
CN107750160B (zh) * 2015-06-09 2021-06-22 百缮药业(苏州)有限公司 氟代环戊烯基胞嘧啶的用途及制备方法

Also Published As

Publication number Publication date
EP3378855B1 (en) 2022-03-09
EP3246320A1 (en) 2017-11-22
EP3246320B1 (en) 2019-05-08
CN110483413B (zh) 2023-02-28
US20140275537A1 (en) 2014-09-18
JP2016519087A (ja) 2016-06-30
US20150376142A1 (en) 2015-12-31
US9150520B2 (en) 2015-10-06
ES2913214T3 (es) 2022-06-01
AU2014232502B2 (en) 2017-12-14
JP6334676B2 (ja) 2018-05-30
CN105143191A (zh) 2015-12-09
JP2018090615A (ja) 2018-06-14
US20170158662A1 (en) 2017-06-08
AU2014232502A1 (en) 2015-10-01
CN107474034B (zh) 2020-06-30
CA2904374C (en) 2022-07-19
MX368669B (es) 2019-10-10
EP3378855A1 (en) 2018-09-26
MX2015012300A (es) 2016-07-26
CA2904374A1 (en) 2014-09-18
US9920016B2 (en) 2018-03-20
ES2740801T3 (es) 2020-02-06
WO2014145807A1 (en) 2014-09-18
CN105143191B (zh) 2017-08-25
BR112015023591A2 (pt) 2017-07-18
AU2018253555A1 (en) 2018-11-22
AU2018253555B2 (en) 2019-08-08
KR20150130472A (ko) 2015-11-23
JP6503100B2 (ja) 2019-04-17
AU2017258856B2 (en) 2018-11-08
EP2970147A1 (en) 2016-01-20
BR112015023591B1 (pt) 2023-04-04
CN110483413A (zh) 2019-11-22
AU2017258856A1 (en) 2017-11-30
CA3160553A1 (en) 2014-09-18
ES2678085T3 (es) 2018-08-08
BR122022026659B1 (pt) 2023-05-16
AU2014232502B8 (en) 2018-01-18
AU2014232502A8 (en) 2018-01-18
EP4112604A1 (en) 2023-01-04
CN107474034A (zh) 2017-12-15
US9533958B2 (en) 2017-01-03
EP2970147B1 (en) 2018-05-30

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