DK2753621T3 - Fremgangsmåder og mellemprodukter til fremstilling af en jak-inhibitor - Google Patents

Fremgangsmåder og mellemprodukter til fremstilling af en jak-inhibitor Download PDF

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DK2753621T3
DK2753621T3 DK12770334.6T DK12770334T DK2753621T3 DK 2753621 T3 DK2753621 T3 DK 2753621T3 DK 12770334 T DK12770334 T DK 12770334T DK 2753621 T3 DK2753621 T3 DK 2753621T3
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compound
formula
salt
mixture
acid
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Jiacheng Zhou
Pingli Liu
Ganfeng Cao
Yongzhong Wu
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Incyte Holdings Corp
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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Claims (23)

1. Fremgangsmåde, omfattende omsætning afen forbindelse med formel III:
eller et salt deraf, med en forbindelse med formel IV:
i tilstedeværelse af et reduktionsmiddel for at danne en forbindelse med formel II:
eller et salt deraf, forudsat at reduktionsmidlet ikke er natriumcyanobordeuterid; hvor P1 er en beskyttelsesgruppe.
2. Fremgangsmåden ifølge krav 1, hvor beskyttelsesgruppen er -CH2OCH2CH2Si(CH3)3.
3. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 2, hvor reduktionsmidlet er valgt fra natriumcyanoborhydrid og natriumtriacetoxyborhydrid.
4. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 2, hvor reduktionsmidlet er natriumtriacetoxyborhydrid.
5. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 4, hvor forbindelsen med formel II, III, og IV hver er en fri base.
6. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 5, yderligere omfattende afbeskyttelse af en forbindelse med formel II, eller salt deraf, for at danne en forbindelse med formel I:
eller et salt deraf.
7. Fremgangsmåden ifølge krav 6, hvor afbeskyttelsen omfatter behandling med bortrifluoridetherat, efterfulgt af behandling med vandig ammoniumhydroxid.
8. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 7, hvor fremgangsmåden yderligere omfatter omsætning af forbindelsen med formel I med adipinsyre til dannelse af adipat-salt.
9. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 8, hvor forbindelserne med formel I, II, III, og IV hver er en fri base.
10. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 7, hvor fremgangsmåden yderligere omfatter: (a) opvarme forbindelsen med formel I i methanol ved tilbagestrømning for at få en blanding; (b) efter (a), tilsætte methylisobutylketon til blandingen; (c) efter (b), fjerne en del af opløsningsmidlet ved destillation ved en indre temperatur på 40°C til 50°C for at danne en koncentreret blanding; (d) efter (c), tilsætte methanol til den koncentrerede blanding for at danne en fortyndet blanding; (e) efter (d), opvarme den fortyndede blanding ved tilbagesvaling for at få en blanding; (f) efter (e), tilsætte methylisobutylketon til blandingen; (g) efter (f), fjerne en del af opløsningsmidlet ved destillation ved en indre temperatur på 40°C til 50°C for at danne en koncentreret blanding; (h) efter (g), tilsætte adipinsyre og methanol til den koncentrerede blanding; (i) efter (h), opvarme blandingen ved tilbagestrømning; and (j) efter (i), fjerne en del af opløsningsmidlet ved destillation ved en indre temperatur på 40°C til 50°C for at danne en koncentreret blanding; (k) efter (j), tilsætte heptan til blandingen; og (l) efter (k), omrøre blandingen ved stuetemperatur for at danne adipinsyresaltet af forbindelsen med formel I.
11. Fremgangsmåden ifølge et hvilket som helst af kravene 6 til 10, hvor forbindelsen med formel IV, eller et salt deraf, fremstilles ved en fremgangsmåde omfattende afbeskyttelse af en forbindelse med formel V:
eller et salt deraf.
12. Fremgangsmåden ifølge krav 11, hvor afbeskyttelsen omfatter omsætning med vandig syre.
13. Fremgangsmåden ifølge krav 12, hvor syren er saltsyre.
14. Fremgangsmåden ifølge et hvilket som helst af kravene 11 til 13, hvor forbindelserne med formel I, II, III, IV, og V hver er en fri base.
15. Fremgangsmåden ifølge et hvilket som helst af kravene 11 til 14, hvor forbindelsen med formel V, eller et salt deraf, fremstilles ved en fremgangsmåde omfattende omsætning af en forbindelse med formel VI:
med en forbindelse med formel VII:
i tilstedeværelse af et koblingsmiddel.
16. Fremgangsmåden ifølge krav 15, hvor koblingsmidlet er benzotriazol-l-yloxy-tris(dimethylamino)-phosphonium-hexafluorphosphat (BOP).
17. Fremgangsmåde til fremstilling af en forbindelse med formel IV:
eller et salt deraf, omfattende afbeskyttelse af en forbindelse med formel V:
eller et salt deraf, for at danne en forbindelse med formel IV, eller salt deraf.
18. Fremgangsmåden ifølge krav 17, hvor afbeskyttelsen omfatter omsætning med vandig syre.
19. Fremgangsmåden ifølge krav 18, hvor syren er saltsyre.
20. Fremgangsmåden ifølge et hvilket som helst af kravene 17 til 19, hvor forbindelserne med formel IV og V hver er en fri base.
21. Fremgangsmåde til fremstilling af en forbindelse med formel V:
eller et salt deraf, omfattende omsætning afen forbindelse med formel VI:
eller et salt deraf, med en forbindelse med formel VII: eller et salt deraf, i tilstedeværelse af et koblingsmiddel for at danne forbindelsen med formel V, eller salt deraf.
22. Fremgangsmåden ifølge krav 21, hvor koblingsmidlet er benzotriazol-l-yloxy-tris(dimethylamino)-phosphonium-hexafluorphosphat (BOP).
23. Forbindelse med formel V:
eller et salt deraf.
DK12770334.6T 2011-09-07 2012-09-06 Fremgangsmåder og mellemprodukter til fremstilling af en jak-inhibitor DK2753621T3 (da)

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US201161531896P 2011-09-07 2011-09-07
PCT/US2012/053921 WO2013036611A1 (en) 2011-09-07 2012-09-06 Processes and intermediates for making a jak inhibitor

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EP (1) EP2753621B1 (da)
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CN (1) CN104024256B (da)
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