DK2964650T3 - Fremgangsmåder og mellemprodukter til fremstilling af en jak inhibitor - Google Patents
Fremgangsmåder og mellemprodukter til fremstilling af en jak inhibitor Download PDFInfo
- Publication number
- DK2964650T3 DK2964650T3 DK14712913.4T DK14712913T DK2964650T3 DK 2964650 T3 DK2964650 T3 DK 2964650T3 DK 14712913 T DK14712913 T DK 14712913T DK 2964650 T3 DK2964650 T3 DK 2964650T3
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- DK
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- Prior art keywords
- compound
- formula
- salt
- azetidin
- pyrrolo
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/14—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 three or more hetero rings
-
- 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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
- B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
- B01J31/26—Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups B01J31/02 - B01J31/24
- B01J31/28—Catalysts comprising hydrides, coordination complexes or organic compounds containing in addition, inorganic metal compounds not provided for in groups B01J31/02 - B01J31/24 of the platinum group metals, iron group metals or copper
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
-
- 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 System
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- 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 System
- C07F5/02—Boron compounds
- C07F5/04—Esters of boric acids
Claims (15)
1. Fremgangsmåde til fremstilling afen forbindelse med formel I: eller et salt deraf, omfattende at: omsætte en forbindelse med formel Illa:
med en forbindelse med formel IVa:
IVa under Suzuki-koblingsbetingelser for at danne en forbindelse med formel
Ila; afbeskytte forbindelsen med formel Ila ved omsætning med hydrogenchlorid for at danne 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl)azetidin-3-yl)acetonitril-dihydrochloridsalt; og omsætte 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl)azetidin-3-yl)acetonitril-dihydrochloridsaltet med en forbindelse med formel VI:
VT i tilstedeværelse af et reduktionsmiddel for at danne en forbindelse med formel I, eller et salt deraf.
2. Fremgangsmåden ifølge krav 1, hvor Suzuki-koblingsbetingelserne omfatter opvarmning af en reaktionsblanding omfattende forbindelsen med formel Illa, forbindelsen med formel IVa, en Suzuki-koblingskatalysator, en base og en opløsningsmiddelkomponent.
3. Fremgangsmåden ifølge krav 2, hvor Suzuki-koblingskatalysatoren er: (a) Pd(dppf)2Cl2, [l,l'-bis(dicyclohexylphosphino)ferrocen]dichlorpalladium (II), tetrakis(triphenylphosphin)palladium(0), eller tetrakis(tri(o-tolyl)phosphin)palladium(O); eller
(b) [l,l'-bis(dicyclohexylphosphino)ferrocene]dichlorpalladium (II).
4. Fremgangsmåden ifølge et hvilket som helst af kravene 2 til 3, hvor basen er: (a) natriumcarbonat, kaliumcarbonat, eller cæciumfluorid; eller (b) cæciumfluorid.
5. Fremgangsmåden ifølge krav 4, hvor basen er cæciumfluorid og er til stede i 3 ækvivalenter eller derover baseret på forbindelsen med formel IVa.
6. Fremgangsmåden ifølge et hvilket som helst af kravene 2 til 5, hvor opløsningsmiddelkomponenten omfatter tert- buta nol og vand.
7. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 6, hvor forbindelserne med formel Illa og IVa er til stede i ca. et 1:1 molærforhold.
8. Fremgangsmåden ifølge krav 1, hvor hydrogenchlorid er til stede i en mængde på 5 til 8 ækvivalenter baseret på forbindelsen med formel Ila.
9. Fremgangsmåden ifølge krav 1 til 8, hvor omsætningen af 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl)azetidin-3-yl)acetonitril-dihydrochloridsalt med en forbindelse med formel VI udføres i tilstedeværelse af mindst to ækvivalenter af en anden base.
10. Fremgangsmåden ifølge krav 9, hvor den anden base er: (a) en tertiær amin; eller (b) triethylamin.
11. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 10, hvor reduktionsmidlet er: (a) natriumcyanoborohydrid eller natriumtriacetoxyborhydrid; eller (b) natriumtriacetoxyborhydrid.
12. Fremgangsmåden ifølge krav 11, hvor reduktionsmidlet er natriumtriacetoxyborhydrid og større end 1 ækvivalent af natriumtriacetoxyborhydrid anvendes baseret på 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl)azetidin-3-yl)acetonitril-dihydrochloridsalt.
13. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 12, hvor større end 1 ækvivalent af forbindelsen med formel VI anvendes baseret på 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl)azetidin-3-yl)acetonitril-dihydrochloridsalt.
14. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 13, hvor omsætningen af 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl)azetidin-3-yl)acetonitril-dihydrochloridsalt med en forbindelse med formel VI udføres i et dichlormethanopløsningsmiddel.
15. Fremgangsmåden ifølge et hvilket som helst af kravene 1 til 14, yderligere omfattende omsætning af forbindelsen med formel I med adipinsyre for at danne adipinsaltet af forbindelsen med formel I.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361773659P | 2013-03-06 | 2013-03-06 | |
PCT/US2014/020554 WO2014138168A1 (en) | 2013-03-06 | 2014-03-05 | Processes and intermediates for making a jak inhibitor |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2964650T3 true DK2964650T3 (da) | 2019-02-11 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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DK14712913.4T DK2964650T3 (da) | 2013-03-06 | 2014-03-05 | Fremgangsmåder og mellemprodukter til fremstilling af en jak inhibitor |
Country Status (35)
Country | Link |
---|---|
US (3) | US8987443B2 (da) |
EP (3) | EP2964650B1 (da) |
JP (2) | JP6397831B2 (da) |
KR (2) | KR102236232B1 (da) |
CN (1) | CN105189509B (da) |
AR (2) | AR095018A1 (da) |
AU (1) | AU2014225938B2 (da) |
BR (2) | BR122021015061B1 (da) |
CA (2) | CA3091179C (da) |
CL (2) | CL2015002468A1 (da) |
CR (2) | CR20190518A (da) |
CY (2) | CY1121512T1 (da) |
DK (1) | DK2964650T3 (da) |
EA (2) | EA030705B1 (da) |
ES (2) | ES2900492T3 (da) |
HK (1) | HK1218540A1 (da) |
HR (2) | HRP20211922T1 (da) |
HU (2) | HUE057262T2 (da) |
IL (3) | IL240891A0 (da) |
LT (2) | LT2964650T (da) |
ME (1) | ME03350B (da) |
MX (2) | MX2015011667A (da) |
NZ (2) | NZ749437A (da) |
PE (2) | PE20151902A1 (da) |
PH (1) | PH12015501958B1 (da) |
PL (2) | PL3489239T3 (da) |
PT (2) | PT3489239T (da) |
RS (2) | RS58547B1 (da) |
SG (2) | SG11201506758RA (da) |
SI (2) | SI2964650T1 (da) |
TR (1) | TR201820520T4 (da) |
TW (1) | TWI634121B (da) |
UA (2) | UA121532C2 (da) |
WO (1) | WO2014138168A1 (da) |
ZA (1) | ZA201908345B (da) |
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