FI68612C - Foerfarande foer framstaellning av antibakteriellt och/eller antimalariskt aktiva 2,4 -diamino-5-bensylpyrimidiner samt vi foerfarandet anvaendbar bensylcyanacetal - Google Patents
Foerfarande foer framstaellning av antibakteriellt och/eller antimalariskt aktiva 2,4 -diamino-5-bensylpyrimidiner samt vi foerfarandet anvaendbar bensylcyanacetal Download PDFInfo
- Publication number
- FI68612C FI68612C FI771816A FI771816A FI68612C FI 68612 C FI68612 C FI 68612C FI 771816 A FI771816 A FI 771816A FI 771816 A FI771816 A FI 771816A FI 68612 C FI68612 C FI 68612C
- Authority
- FI
- Finland
- Prior art keywords
- benzyl
- cyanoacetal
- formula
- group
- diamino
- Prior art date
Links
Classifications
-
- 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
- C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01G—HORTICULTURE; CULTIVATION OF VEGETABLES, FLOWERS, RICE, FRUIT, VINES, HOPS OR SEAWEED; FORESTRY; WATERING
- A01G5/00—Floral handling
- A01G5/04—Mountings for wreaths, or the like; Racks or holders for flowers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C67/00—Preparation of carboxylic acid esters
- C07C67/27—Preparation of carboxylic acid esters from ortho-esters
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Environmental Sciences (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (19)
1. Vid framställning av antibakteriellt och/eller antima-lariskt aktiva 2,4-diamino-5-bensylpyrimidiner med formeln (XI) R1 H „ CH? WH2 <XI) användbar bensylcyanacetal med formeln (I) , CN R1 I 4 v-\/ch2-c-r r (I) r2________Yn CH(ORj)2 r3x>0" 12 3 varvid R , R och R är lika eller olika och var och en är en halogen- ellei? väteatom, en alkoxi-, alkyl- eller dialkylaminogrupp, 4 5 R är en alkoxikarbonyl- eller aldehydgrupp, och R är en alkyl- grupp, varvid alkyl- eller alkoxigrupperna var och en har 1-4 kolat omer.
2. Bensylcyanacetal enligt patentkravet 1, k ä n n e t e c k- 12 3 n a d därav, att R , R och R är lika eller olika och var och en är en metyl- eller metoxigrupp eller en väteatom.
3. Bensylcyanacetal enligt patentkravet 2,känneteck- 12 3 n a d därav, att R , R och R är metoxigrupper substituerade i 3-, 4- och 5-ställningen av fenylringen.
4. Bensylcyanacetal enligt patentkravet 2,känneteck- 1 2 n a d därav, att R och R är metoxigrupper substituerade 1-, 3- 3 och 4-ställnmgen av fenylringen och R är en väteatom.
5. Bensylcyanacetal enligt patentkravet 2,känneteck- n a d därav, att R är en metylgrupp substituerad i 2-ställningen 2 3 av fenylringen och R och R är metoxigrupper substituerade i 4-och 5-ställningen av fenylringen.
6. Bensylcyanacetal enligt patentkravet 1, känneteck-n a d därav, att R4 är en metoxikarbonylgrupp. 6861 2 18
7. Bensylcyanacetal enligt patentkravet 1, kannelee k- - 4 n a d. därav, att R är en etoxikarbonylgrupp.
8. Bensylcyanacetal enligt patentkravet 1 , k ä n n e t e c k-n a d därav, att R är en butoxikarbonylgrupp.
9. Bensylcyanacetal enligt nägot av föregaende patentkrav, 5 kannetecknad därav, att R är en metyl- eller etyl-grupp.
10. Bensylcyanacetal enligt patentkravet 1, kannetecknad därav, att den är ^-dimetoximetyl-o(-formyl-/> -( 3 ,4 , 5-tri-metoxifenyl)propionitril.
11. Bensylcyanacetal enligt patentkravet 1, känneteck-n a d därav, att den ärS.-dietoximetyl-o(-formyl-/^-(3,4,5-tri-metoxifeny1)propionitril.
12. Bensylcyanacetal enligt patentkravet 1, kannetecknad därav, att den är -karbetoxi- °( -die toximety 1- β - ( 3 , 4 , 5-tri-metoxifenyDpropionitril.
13. Förfarande för framställning av antibakteriellt och/eller antimalariskt aktiva 2,4-diamino-5-bensylpyrimidiner med formeln (XI): R1 f H2NV_n "''TO)- CH2 -\0)-NH2 R^ kännetecknat därav, att man omsätter en bensylcyanacetal med formeln (I): R1 CN ' 4 x CH„-C-R ^ 2 | Λ , (I) R2 f r CHCOR )„ 2 3 4 5 2 varvid R , R , R , R och R betecknar samma som i patentkravet 1, med guanidin i ett lösningsmedel som är kapabelt att lösa bagge reaktanterna.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB2375676 | 1976-06-09 | ||
GB23756/76A GB1582245A (en) | 1976-06-09 | 1976-06-09 | Benzyl cyanoacetal derivatives and their conversion to pyrimidine derivatives |
Publications (3)
Publication Number | Publication Date |
---|---|
FI771816A FI771816A (sv) | 1977-12-10 |
FI68612B FI68612B (fi) | 1985-06-28 |
FI68612C true FI68612C (fi) | 1985-10-10 |
Family
ID=10200818
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI771816A FI68612C (fi) | 1976-06-09 | 1977-06-08 | Foerfarande foer framstaellning av antibakteriellt och/eller antimalariskt aktiva 2,4 -diamino-5-bensylpyrimidiner samt vi foerfarandet anvaendbar bensylcyanacetal |
Country Status (19)
Country | Link |
---|---|
US (2) | US4144263A (sv) |
JP (2) | JPS5826908B2 (sv) |
AT (1) | AT350537B (sv) |
AU (1) | AU510298B2 (sv) |
BE (1) | BE855505A (sv) |
CA (2) | CA1091672A (sv) |
CH (1) | CH632239A5 (sv) |
DE (1) | DE2725992C2 (sv) |
DK (1) | DK254077A (sv) |
FI (1) | FI68612C (sv) |
FR (1) | FR2354317A1 (sv) |
GB (1) | GB1582245A (sv) |
GR (1) | GR63824B (sv) |
HU (2) | HU178138B (sv) |
IL (1) | IL52278A (sv) |
NL (1) | NL172541C (sv) |
NZ (1) | NZ184330A (sv) |
SE (1) | SE7706655L (sv) |
ZA (1) | ZA773466B (sv) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4438267A (en) * | 1980-11-11 | 1984-03-20 | Daluge Susan M | Monoheteroring compounds and their use |
JPS62188328A (ja) * | 1986-02-14 | 1987-08-17 | Toshiba Seiki Kk | ペレツト装着装置 |
JPH01152656A (ja) * | 1987-12-09 | 1989-06-15 | Sanken Electric Co Ltd | リードフレームへのスクリーン印刷方法 |
FI895821A0 (fi) * | 1988-12-07 | 1989-12-05 | Wellcome Found | Farmaceutiskt aktiva cns foereningar. |
PL1725540T3 (pl) | 2004-03-05 | 2013-02-28 | Hoffmann La Roche | Diaminopirymidyny jako antagoniści p2x3 i p2x2/3 |
ES2562056T3 (es) * | 2005-09-01 | 2016-03-02 | F. Hoffmann-La Roche Ag | Diaminopirimidinas como moduladores P2X3 y P2X2/3 |
WO2007025899A1 (en) * | 2005-09-01 | 2007-03-08 | F. Hoffmann-La Roche Ag | Diaminopyrimidines as p2x3 and p2x2/3 modulators |
AU2006286576B2 (en) * | 2005-09-01 | 2012-06-14 | F. Hoffmann-La Roche Ag | Diaminopyrimidines as P2X3 and P3X2/3 modulators |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2755298A (en) * | 1956-07-17 | pwiiq | ||
US2579259A (en) * | 1951-12-18 | Iamino-s- | ||
US2576939A (en) * | 1951-12-04 | -diamino-s-phenyl-e-alkyl- | ||
US3485840A (en) * | 1964-11-12 | 1969-12-23 | Hoffmann La Roche | 2,4-diamino - 5 - (2',4',5'-substituted benzyl) pyrimidines,intermediates and processes |
GB1142654A (en) * | 1965-10-28 | 1969-02-12 | Wellcome Found | Cyano-acetals and their use in benzylpyrimidine synthesis |
US3772289A (en) * | 1970-10-22 | 1973-11-13 | Burroughs Wellcome Co | Alkyl substituted benzyl pyrimidines |
BE795023A (fr) * | 1972-02-07 | 1973-08-06 | Hoffmann La Roche | Nouvelles benzylpyrimidines |
-
1976
- 1976-06-09 GB GB23756/76A patent/GB1582245A/en not_active Expired
-
1977
- 1977-06-08 FI FI771816A patent/FI68612C/fi not_active IP Right Cessation
- 1977-06-08 DE DE2725992A patent/DE2725992C2/de not_active Expired
- 1977-06-08 US US05/804,537 patent/US4144263A/en not_active Expired - Lifetime
- 1977-06-08 BE BE178296A patent/BE855505A/xx not_active IP Right Cessation
- 1977-06-08 NZ NZ184330A patent/NZ184330A/xx unknown
- 1977-06-08 DK DK254077A patent/DK254077A/da not_active Application Discontinuation
- 1977-06-08 ZA ZA00773466A patent/ZA773466B/xx unknown
- 1977-06-08 FR FR7717526A patent/FR2354317A1/fr active Granted
- 1977-06-08 NL NLAANVRAGE7706284,A patent/NL172541C/xx not_active IP Right Cessation
- 1977-06-08 CH CH706277A patent/CH632239A5/de not_active IP Right Cessation
- 1977-06-08 IL IL52278A patent/IL52278A/xx unknown
- 1977-06-08 HU HU77WE602A patent/HU178138B/hu unknown
- 1977-06-08 GR GR53658A patent/GR63824B/el unknown
- 1977-06-08 HU HU77WE561A patent/HU178806B/hu unknown
- 1977-06-08 JP JP52066788A patent/JPS5826908B2/ja not_active Expired
- 1977-06-08 AT AT405777A patent/AT350537B/de not_active IP Right Cessation
- 1977-06-08 CA CA280,134A patent/CA1091672A/en not_active Expired
- 1977-06-08 SE SE7706655A patent/SE7706655L/sv not_active Application Discontinuation
- 1977-06-08 AU AU25917/77A patent/AU510298B2/en not_active Expired
-
1978
- 1978-11-24 US US05/963,399 patent/US4216319A/en not_active Expired - Lifetime
-
1980
- 1980-03-25 CA CA348,327A patent/CA1091673A/en not_active Expired
-
1982
- 1982-01-05 JP JP57000543A patent/JPS6049633B2/ja not_active Expired
Also Published As
Publication number | Publication date |
---|---|
US4144263A (en) | 1979-03-13 |
NL7706284A (nl) | 1977-12-13 |
GB1582245A (en) | 1981-01-07 |
FR2354317A1 (fr) | 1978-01-06 |
FR2354317B1 (sv) | 1980-02-01 |
HU178138B (en) | 1982-03-28 |
CH632239A5 (de) | 1982-09-30 |
US4216319A (en) | 1980-08-05 |
JPS52151145A (en) | 1977-12-15 |
ATA405777A (de) | 1978-11-15 |
SE7706655L (sv) | 1977-12-10 |
GR63824B (en) | 1979-12-19 |
HU178806B (en) | 1982-06-28 |
FI68612B (fi) | 1985-06-28 |
IL52278A (en) | 1981-07-31 |
NL172541B (nl) | 1983-04-18 |
JPS6049633B2 (ja) | 1985-11-02 |
DE2725992A1 (de) | 1977-12-29 |
BE855505A (fr) | 1977-12-08 |
ZA773466B (en) | 1978-04-26 |
JPS5826908B2 (ja) | 1983-06-06 |
JPS57136577A (en) | 1982-08-23 |
IL52278A0 (en) | 1977-08-31 |
NZ184330A (en) | 1979-03-28 |
NL172541C (nl) | 1983-09-16 |
FI771816A (sv) | 1977-12-10 |
AT350537B (de) | 1979-06-11 |
DK254077A (da) | 1977-12-10 |
DE2725992C2 (de) | 1983-02-17 |
AU510298B2 (en) | 1980-06-19 |
AU2591777A (en) | 1978-12-14 |
CA1091672A (en) | 1980-12-16 |
CA1091673A (en) | 1980-12-16 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
MM | Patent lapsed |
Owner name: THE WELLCOME FOUNDATION LIMITED |