FI106461B - Förfarande för framställning av terapeutiskt användbara enantiomeriska föreningar samt vid förfarandet användbar mellanprodukt - Google Patents
Förfarande för framställning av terapeutiskt användbara enantiomeriska föreningar samt vid förfarandet användbar mellanprodukt Download PDFInfo
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- FI106461B FI106461B FI906367A FI906367A FI106461B FI 106461 B FI106461 B FI 106461B FI 906367 A FI906367 A FI 906367A FI 906367 A FI906367 A FI 906367A FI 106461 B FI106461 B FI 106461B
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- methanol
- compound
- salt
- amino
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic 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
- C07D239/28—Heterocyclic 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
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/42—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups or hydroxy groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic 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
- C07D239/28—Heterocyclic 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic 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
- C07D239/28—Heterocyclic 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic 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
- C07D239/28—Heterocyclic 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/50—Three nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
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- 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
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated
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Claims (5)
1. Förfarande för framställning av terapeutiskt an-vändbara enantiomeriska föreningar med den allmänna formeln 5 Jy\
10 H2N^N (i) A väri R är en cyklopropylamino- eller N-cyklopropyl-N-15 metylaminogrupp och A är en 2-cyklopenten-l-metanol-4-ylgrupp i (IS,4R)-konfiguration, samt deras salter eller estrar, eller salter av estrar, varvid nämnda föreningar och deras salter eller estrar, eller salter av estrar, en-var förligger i form av en enantiomer, väsentligen fri frän 20 motenantiomer, kännetecknat av att A) en enantiomerförening med formeln £ : .· 25 k JL / • · · Δ I ::: a • · • » s'·'·' där A är en i det föregäende definierad grupp och Z är en • · · prekursorgrupp tili den i samband med formeln I definierade 30 gruppen R, eller ett sait eller en ester, eller ett sait av • · *···1 en ester, av densamma, behandlas med ett ämne eller vid be- • · · ...1 tingelser, vilka ästadkommer att prekursorgruppen Z omvand- ·;··· las tili en önskad grupp R; eller • · • · · « · « • · · « · t • · » 61 106461 B) en enantiomer förening med formeln R N ,-
5 JL (HI) R3Nlf^N ^NH A där A och R är i det föregäende definierade grupper, R2 är väte eller en formylgrupp och R3 är en aminoskyddsgrupp, 10 ett salt eller ester, eller ett salt av en ester, av den-samma, omsätts med ett ämne, som ästadkommer att en imidat-soliring bildas i den önskade föreningen med formeln I och att aminoskyddsgruppen R3 avlägsnas; eller C) enantiomerförening med formeln 15 1. ii / (IV) r3nh'^n'^^ 20 a där A och R är i det föregäende definierade grupper och R3 : är en aminos kyddsgrupp, eller ett salt eller en ester, el- < : ler ett salt av en ester, av densamma, omsätts med ett ämne 1 ' ; 25 som ästadkommer att skyddsgruppen R3 avlägsnas, och möjli- • ♦ j j*j gen utförs den ena eller bägge av följande omvandlingar i • I» .···, vilken som heist önskad följd: I·· i) när en förening med formeln I har bildats, om-vandlas den nämnda föreningen till ett salt eller en ester, 30 eller ett salt av en ester; eller ♦ · *···* ii) när ett salt eller en ester, eller ett salt av • · · • · ···* en ester av föreningar med formeln I har bildats, omvandlas ·;··· detta respektive denna till en utgängsförening med formeln ....: I eller till ett salt eller en ester, eller ett salt av en • 35 ester. « · 4 4 4 ♦ 4 ♦ 1 φ 4 4 4 • 4 4 4 4 62 106461
2. Förfarande enligt patentkrav 1, kanne-tecknat av att man framställer (IS,4R)-cis-4- [2-amino-6-(cyklopropylamino)-9H-purin-9-yl]-2-cyklopenten-l-metanol, i form som är väsentligen fri frän motsvarande 5 (1R, 4S)-enantiomer.
3. Förfarande enligt patentkrav 1, känne- t e c k n a t, av att man framställer (IS, 4R) -cis-4-[2-amino-6-(N-cyklopropyl-N-metylamino)-9H-purin-9-yl]-2-cyklopenten-l-metanol, i form som är väsentligen fri frän 10 motsvarande (1R,4S)-enantiomer.
4. Förfarande enligt patentkrav 1 för framställning av farmaceutiskt godtagbara salter, estrar och salter av estrar, av (IS,4R)-enantiomera föreningar.
5. Förening som är användbar säsom mellanprodukt vid 15 framställning av föreningar med formeln I medelst förfarande C i patentkrav 1 och som har formeln N^Sr/\ | I x) (IV) 20 ,¾ A» A ; där A är 2-cyklopenten-l-metanol-4-yl i (1S,4R)~ * konfiguration, R3 är en Ci-g-alkanoylgrupp och R är en cyk- . 25 lopropylamino- eller N-cyklopropyl-N-metylaminogrupp. • · • · « « · · • · · • · · • · • · · * · · • · · « · · • · · : : j • · · • · · • ♦ ♦ · ♦ t « « · < < i t • M M • ·
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FI970666A FI105813B (sv) | 1989-12-22 | 1997-02-17 | Enantiomeriska mellanprodukter |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US45520189 | 1989-12-22 | ||
US07/455,201 US5034394A (en) | 1988-06-27 | 1989-12-22 | Therapeutic nucleosides |
Publications (3)
Publication Number | Publication Date |
---|---|
FI906367A0 FI906367A0 (fi) | 1990-12-21 |
FI906367A FI906367A (fi) | 1991-06-23 |
FI106461B true FI106461B (sv) | 2001-02-15 |
Family
ID=23807819
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI906367A FI106461B (sv) | 1989-12-22 | 1990-12-21 | Förfarande för framställning av terapeutiskt användbara enantiomeriska föreningar samt vid förfarandet användbar mellanprodukt |
FI20001175A FI20001175A (sv) | 1989-12-22 | 2000-05-16 | Enantiomeriska föreningar som är väsentligen fria från motverkande enentiomerer |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI20001175A FI20001175A (sv) | 1989-12-22 | 2000-05-16 | Enantiomeriska föreningar som är väsentligen fria från motverkande enentiomerer |
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EP (3) | EP0921121A1 (sv) |
JP (2) | JPH11158160A (sv) |
CN (1) | CN1028106C (sv) |
AP (1) | AP196A (sv) |
AT (1) | ATE181917T1 (sv) |
AU (1) | AU633672B2 (sv) |
CA (1) | CA2033044C (sv) |
CY (1) | CY2145B1 (sv) |
CZ (1) | CZ283481B6 (sv) |
DE (2) | DE69033197T2 (sv) |
DK (1) | DK0434450T3 (sv) |
ES (1) | ES2133138T3 (sv) |
FI (2) | FI106461B (sv) |
GR (1) | GR3031100T3 (sv) |
HK (1) | HK1009600A1 (sv) |
HU (3) | HU219454B (sv) |
IE (3) | IE990826A1 (sv) |
IL (1) | IL96748A (sv) |
LU (1) | LU90426I2 (sv) |
MX (1) | MX9203215A (sv) |
MY (1) | MY104575A (sv) |
NL (1) | NL990028I2 (sv) |
NZ (1) | NZ236593A (sv) |
PL (1) | PL167097B1 (sv) |
PT (1) | PT96321B (sv) |
RU (2) | RU2068849C1 (sv) |
SG (1) | SG49685A1 (sv) |
SK (2) | SK280216B6 (sv) |
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CN104788451A (zh) * | 2014-01-21 | 2015-07-22 | 浙江九洲药业股份有限公司 | 一种阿巴卡韦的制备方法 |
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EP0366385B1 (en) * | 1988-10-24 | 1993-06-09 | The Wellcome Foundation Limited | Guanine derivatives having antiviral activity and their pharmaceutically acceptable salts |
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US4939252A (en) * | 1989-04-20 | 1990-07-03 | Hoffmann-La Roche Inc. | Novel intermediates for the preparation of Carbovir |
-
1990
- 1990-12-20 MY MYPI90002230A patent/MY104575A/en unknown
- 1990-12-21 ZA ZA9010365A patent/ZA9010365B/xx unknown
- 1990-12-21 CA CA002033044A patent/CA2033044C/en not_active Expired - Lifetime
- 1990-12-21 SK SK6583-90A patent/SK280216B6/sk not_active IP Right Cessation
- 1990-12-21 FI FI906367A patent/FI106461B/sv active Protection Beyond IP Right Term
- 1990-12-21 PT PT96321A patent/PT96321B/pt not_active IP Right Cessation
- 1990-12-21 CZ CS906583A patent/CZ283481B6/cs not_active IP Right Cessation
- 1990-12-21 RU SU904894161A patent/RU2068849C1/ru active
- 1990-12-21 HU HU407/90A patent/HU219454B/hu unknown
- 1990-12-21 EP EP99103525A patent/EP0921121A1/en not_active Withdrawn
- 1990-12-21 AP APAP/P/1990/000234A patent/AP196A/en active
- 1990-12-21 ES ES90314089T patent/ES2133138T3/es not_active Expired - Lifetime
- 1990-12-21 IE IE19990826A patent/IE990826A1/en unknown
- 1990-12-21 DE DE69033197T patent/DE69033197T2/de not_active Expired - Lifetime
- 1990-12-21 AT AT90314089T patent/ATE181917T1/de active
- 1990-12-21 IE IE465290A patent/IE904652A1/en not_active IP Right Cessation
- 1990-12-21 EP EP90314089A patent/EP0434450B1/en not_active Expired - Lifetime
- 1990-12-21 HU HU9902539A patent/HU220067B/hu unknown
- 1990-12-21 HU HU9902543A patent/HU220630B1/hu unknown
- 1990-12-21 AU AU68419/90A patent/AU633672B2/en not_active Expired
- 1990-12-21 EP EP99103526A patent/EP0921114A1/en not_active Withdrawn
- 1990-12-21 PL PL90288403A patent/PL167097B1/pl unknown
- 1990-12-21 DE DE1990633197 patent/DE19975058I1/de active Pending
- 1990-12-21 NZ NZ236593A patent/NZ236593A/en unknown
- 1990-12-21 IE IE19990825A patent/IE990825A1/en unknown
- 1990-12-21 SG SG1996004082A patent/SG49685A1/en unknown
- 1990-12-21 DK DK90314089T patent/DK0434450T3/da active
- 1990-12-21 CN CN91100671A patent/CN1028106C/zh not_active Expired - Lifetime
- 1990-12-21 IL IL9674890A patent/IL96748A/en not_active IP Right Cessation
-
1991
- 1991-04-09 TW TW080102699A patent/TW371660B/zh not_active IP Right Cessation
- 1991-04-09 TW TW088111311A patent/TW473466B/zh not_active IP Right Cessation
-
1992
- 1992-06-04 RU SU925011830A patent/RU2091386C1/ru active
- 1992-06-24 MX MX9203215A patent/MX9203215A/es active IP Right Grant
- 1992-08-10 SK SK2470-92A patent/SK247092A3/sk not_active IP Right Cessation
-
1998
- 1998-08-31 HK HK98110320A patent/HK1009600A1/xx not_active IP Right Cessation
- 1998-09-28 JP JP10273408A patent/JPH11158160A/ja active Pending
-
1999
- 1999-05-06 JP JP11126185A patent/JPH11343292A/ja active Pending
- 1999-08-06 LU LU90426C patent/LU90426I2/fr unknown
- 1999-08-26 GR GR990402183T patent/GR3031100T3/el unknown
- 1999-09-14 NL NL990028C patent/NL990028I2/nl unknown
- 1999-12-09 CY CY9900044A patent/CY2145B1/xx unknown
-
2000
- 2000-05-16 FI FI20001175A patent/FI20001175A/sv unknown
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Owner name: THE WELLCOME FOUNDATION LIMITED |
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Spc suppl protection certif: L190 Extension date: 20140627 |