ME02846B - Postupak za kristalizaciju (s) - izopropil 2- (((s) - (perfluorofenoksi)( fenoksi)fosforil)amino) propanoata - Google Patents
Postupak za kristalizaciju (s) - izopropil 2- (((s) - (perfluorofenoksi)( fenoksi)fosforil)amino) propanoataInfo
- Publication number
- ME02846B ME02846B MEP-2017-196A MEP19617A ME02846B ME 02846 B ME02846 B ME 02846B ME P19617 A MEP19617 A ME P19617A ME 02846 B ME02846 B ME 02846B
- Authority
- ME
- Montenegro
- Prior art keywords
- perfluorophenoxy
- propanoate
- phosphoryl
- phenoxy
- pyridine
- Prior art date
Links
- -1 Nucleoside phosphoramidates Chemical class 0.000 title 1
- 239000002777 nucleoside Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 claims 8
- 238000000034 method Methods 0.000 claims 7
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 claims 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 4
- 239000007788 liquid Substances 0.000 claims 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- 238000002425 crystallisation Methods 0.000 claims 3
- 230000008025 crystallization Effects 0.000 claims 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims 3
- 230000000269 nucleophilic effect Effects 0.000 claims 3
- MIILDBHEJQLACD-ZJPIPACBSA-N propan-2-yl (2s)-2-[[(2,3,4,5,6-pentafluorophenoxy)-phenoxyphosphoryl]amino]propanoate Chemical compound O([P@@](=O)(N[C@@H](C)C(=O)OC(C)C)OC=1C(=C(F)C(F)=C(F)C=1F)F)C1=CC=CC=C1 MIILDBHEJQLACD-ZJPIPACBSA-N 0.000 claims 3
- RKMGAJGJIURJSJ-UHFFFAOYSA-N 2,2,6,6-tetramethylpiperidine Chemical compound CC1(C)CCCC(C)(C)N1 RKMGAJGJIURJSJ-UHFFFAOYSA-N 0.000 claims 2
- VHYFNPMBLIVWCW-UHFFFAOYSA-N 4-Dimethylaminopyridine Chemical compound CN(C)C1=CC=NC=C1 VHYFNPMBLIVWCW-UHFFFAOYSA-N 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical group [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims 2
- SGUVLZREKBPKCE-UHFFFAOYSA-N 1,5-diazabicyclo[4.3.0]-non-5-ene Chemical compound C1CCN=C2CCCN21 SGUVLZREKBPKCE-UHFFFAOYSA-N 0.000 claims 1
- YFOOEYJGMMJJLS-UHFFFAOYSA-N 1,8-diaminonaphthalene Chemical compound C1=CC(N)=C2C(N)=CC=CC2=C1 YFOOEYJGMMJJLS-UHFFFAOYSA-N 0.000 claims 1
- VSTXCZGEEVFJES-UHFFFAOYSA-N 1-cycloundecyl-1,5-diazacycloundec-5-ene Chemical compound C1CCCCCC(CCCC1)N1CCCCCC=NCCC1 VSTXCZGEEVFJES-UHFFFAOYSA-N 0.000 claims 1
- XBNGYFFABRKICK-UHFFFAOYSA-N 2,3,4,5,6-pentafluorophenol Chemical compound OC1=C(F)C(F)=C(F)C(F)=C1F XBNGYFFABRKICK-UHFFFAOYSA-N 0.000 claims 1
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 239000012296 anti-solvent Substances 0.000 claims 1
- FJDQFPXHSGXQBY-UHFFFAOYSA-L caesium carbonate Chemical compound [Cs+].[Cs+].[O-]C([O-])=O FJDQFPXHSGXQBY-UHFFFAOYSA-L 0.000 claims 1
- 229910000024 caesium carbonate Inorganic materials 0.000 claims 1
- UAOMVDZJSHZZME-UHFFFAOYSA-N diisopropylamine Chemical compound CC(C)NC(C)C UAOMVDZJSHZZME-UHFFFAOYSA-N 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- IZUPBVBPLAPZRR-UHFFFAOYSA-N pentachloro-phenol Natural products OC1=C(Cl)C(Cl)=C(Cl)C(Cl)=C1Cl IZUPBVBPLAPZRR-UHFFFAOYSA-N 0.000 claims 1
- 229910000027 potassium carbonate Inorganic materials 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- MIILDBHEJQLACD-KPORQTCDSA-N propan-2-yl (2s)-2-[[(2,3,4,5,6-pentafluorophenoxy)-phenoxyphosphoryl]amino]propanoate Chemical compound FC=1C(F)=C(F)C(F)=C(F)C=1OP(=O)(N[C@@H](C)C(=O)OC(C)C)OC1=CC=CC=C1 MIILDBHEJQLACD-KPORQTCDSA-N 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- SBYHFKPVCBCYGV-UHFFFAOYSA-N quinuclidine Chemical compound C1CC2CCN1CC2 SBYHFKPVCBCYGV-UHFFFAOYSA-N 0.000 claims 1
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- IMNIMPAHZVJRPE-UHFFFAOYSA-N triethylenediamine Chemical compound C1CN2CCN1CC2 IMNIMPAHZVJRPE-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (7)
- l. Postupak za pripremu kristalnog (S)-izopropil 2-(((S)-(perfluorofenoksi)(fenoksi)fosforil)amino)propanoata koji je predstavljen formulomkoji sadrži:kristalizaciju (S)-izopropil 2-(((S)-(perfluorofenoksi)(fenoksi)fosforil)amino)propanoata od druge kompozicije koja sadrži a) prvu kompoziciju;b) pentafluorofenol;c) ne-nukleofilnu bazu; i d) tečnu kompoziciju;gde prva kompozicija sadrži (S)-izopropil 2-(((S)-(perfluorofenoksi)(fenoksi)fosforil)amino)propanoat i (S)-izopropil 2-(((R)-(perfluorofenoksi)(fenoksi)fosforil )amino) propanoat, i gde tečn a kompozicija sadrži najmanje j edan od rastv arača i anti-rastvarača .
- 2. Postupak iz patentnog zahteva l, u kome se kristalizacija odigrava na temperaturi koja je u opsegu od -10°C do +40°C.
- 3. Postupak IZ patentnog zahteva 2, u kome se kristalizacija odigrava na sobnoj temperaturi.
- 4. Postupak iz patentnog zahteva 1, u kome je ne-nukleofilna baza odabrana između kalijum karbonata, cezijum karbonata, di-izopropilamina, diizopropiletilamina, trietilamina, hinuklidina, naftalen-1,8-diamina, 2,2,6,6-tetrametilpiperidina, 1,8-diazabicikloundec-7-ena,4-dimetilamino-piridina, piridina, 2,6-di-C1-6-alkil-piridina, 2,4,6-tri-C 1-6-alkil-piridina, 1,5-diazabiciklo[4.3.0]non-5-ena, 1,4- diazabiciklo[2.2.2]oktana, ili njihovih smeša.
- 5. Postupak iz patentnog zahteva 4, u kome je ne-nukleofilna baza trietilamin.
- 6. Postupak iz patentnog zahteva 1, u kome tečna kompozicija sadrži najmanje jedan od C2 do C8 etra, C3 do C7 estra, i C5 do C12 zasićenog ugljovodonika.
- 7. Postupak iz patentnog zahteva 1, u kome tečna kompozicija sadrži najmanje jedan od etil acetata, t-butil-metiletra, i heksana.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31951310P | 2010-03-31 | 2010-03-31 | |
| US31954810P | 2010-03-31 | 2010-03-31 | |
| US12/783,680 US8642756B2 (en) | 2009-05-20 | 2010-05-20 | Nucleoside phosphoramidates |
| EP13159791.6A EP2609923B1 (en) | 2010-03-31 | 2011-03-31 | Process for the crystallisation of (s)-isopropyl 2-(((s)-(perfluorophenoxy)(phenoxy)phosphoryl)amino)propanoate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02846B true ME02846B (me) | 2018-01-20 |
Family
ID=55359000
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2015-199A ME02294B (me) | 2010-03-31 | 2011-03-31 | Kristalni (s)-izopropil 2-(((s)-(((2r,3r,4r,5r)-5-(2 ,4-dioks0-3,4-dihidropirimidin-1-(2h)-il )-4 - fluor0-3-hidroksi-4-metiltetrahidrofuran-2- il)metoksi)(fenoksi)fosforil)amino)propanoat |
| MEP-2017-196A ME02846B (me) | 2010-03-31 | 2011-03-31 | Postupak za kristalizaciju (s) - izopropil 2- (((s) - (perfluorofenoksi)( fenoksi)fosforil)amino) propanoata |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2015-199A ME02294B (me) | 2010-03-31 | 2011-03-31 | Kristalni (s)-izopropil 2-(((s)-(((2r,3r,4r,5r)-5-(2 ,4-dioks0-3,4-dihidropirimidin-1-(2h)-il )-4 - fluor0-3-hidroksi-4-metiltetrahidrofuran-2- il)metoksi)(fenoksi)fosforil)amino)propanoat |
Country Status (4)
| Country | Link |
|---|---|
| BR (1) | BR122013004621A2 (me) |
| ME (2) | ME02294B (me) |
| RS (1) | RS56229B1 (me) |
| SI (1) | SI2552930T1 (me) |
-
2011
- 2011-03-31 BR BR122013004621A patent/BR122013004621A2/pt not_active Application Discontinuation
- 2011-03-31 ME MEP-2015-199A patent/ME02294B/me unknown
- 2011-03-31 RS RS20170840A patent/RS56229B1/sr unknown
- 2011-03-31 SI SI201130617T patent/SI2552930T1/sl unknown
- 2011-03-31 ME MEP-2017-196A patent/ME02846B/me unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SI2552930T1 (sl) | 2016-02-29 |
| ME02294B (me) | 2016-02-20 |
| BR122013004621A2 (pt) | 2016-11-22 |
| RS56229B1 (sr) | 2017-11-30 |
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