DK125553B - Fremgangsmåde til fremstilling af substituerede 2,4-diamino-5-benzylpyrimidiner. - Google Patents

Fremgangsmåde til fremstilling af substituerede 2,4-diamino-5-benzylpyrimidiner.

Info

Publication number
DK125553B
DK125553B DK554065AA DK554065A DK125553B DK 125553 B DK125553 B DK 125553B DK 554065A A DK554065A A DK 554065AA DK 554065 A DK554065 A DK 554065A DK 125553 B DK125553 B DK 125553B
Authority
DK
Denmark
Prior art keywords
benzylpyrimidines
diamino
substituted
preparation
Prior art date
Application number
DK554065AA
Other languages
Danish (da)
English (en)
Inventor
M Hoffer
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27559952&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DK125553(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of DK125553B publication Critical patent/DK125553B/da

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
    • C07D239/30—Halogen atoms or nitro radicals
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23K—FODDER
    • A23K20/00—Accessory food factors for animal feeding-stuffs
    • A23K20/10—Organic substances
    • A23K20/116—Heterocyclic compounds
    • A23K20/137—Heterocyclic compounds containing two hetero atoms, of which at least one is nitrogen
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • 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
    • 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
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • 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
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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 with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Zoology (AREA)
  • Animal Husbandry (AREA)
  • Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Fodder In General (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
DK554065AA 1964-11-12 1965-10-28 Fremgangsmåde til fremstilling af substituerede 2,4-diamino-5-benzylpyrimidiner. DK125553B (da)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US41079364A 1964-11-12 1964-11-12
US41071064A 1964-11-12 1964-11-12
US45417265A 1965-05-07 1965-05-07
US45416865A 1965-05-07 1965-05-07
US46083465A 1965-06-02 1965-06-02
US470917A US3341541A (en) 1964-11-12 1965-07-09 Processes and intermediates for pyrimidine derivatives

Publications (1)

Publication Number Publication Date
DK125553B true DK125553B (da) 1973-03-05

Family

ID=27559952

Family Applications (2)

Application Number Title Priority Date Filing Date
DK554065AA DK125553B (da) 1964-11-12 1965-10-28 Fremgangsmåde til fremstilling af substituerede 2,4-diamino-5-benzylpyrimidiner.
DK581065AA DK115847B (da) 1964-11-12 1965-11-11 Fremgangsmåde til fremstilling af terapeutisk aktive 2,4-diamino-5-benzyl-pyrimidinderivater eller syreadditionssalte deraf.

Family Applications After (1)

Application Number Title Priority Date Filing Date
DK581065AA DK115847B (da) 1964-11-12 1965-11-11 Fremgangsmåde til fremstilling af terapeutisk aktive 2,4-diamino-5-benzyl-pyrimidinderivater eller syreadditionssalte deraf.

Country Status (15)

Country Link
US (3) US3485840A (ru)
BE (3) BE671983A (ru)
BR (3) BR6574668D0 (ru)
CH (2) CH467784A (ru)
DE (2) DE1545966A1 (ru)
DK (2) DK125553B (ru)
FI (1) FI43251B (ru)
FR (1) FR5411M (ru)
GB (7) GB1132083A (ru)
IL (7) IL24498A (ru)
IT (1) IT1058251B (ru)
MY (2) MY6700159A (ru)
NL (3) NL6514178A (ru)
NO (2) NO115741B (ru)
SE (4) SE311160B (ru)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US3515783A (en) * 1967-10-20 1970-06-02 Hoffmann La Roche Antibacterial composition containing 5-methyl - 3 - sulfanilamidoisoxazole and trimethoxybenzyl pyrimidine
DE2065367C2 (de) * 1969-03-06 1985-04-04 The Wellcome Foundation Ltd., London Verfahren zur Herstellung von 2,4- Diamino-5-benzylpyrimidinen
GB1261455A (en) * 1969-03-06 1972-01-26 Burroughs Wellcome Co Improvements in or relating to substituted acrylonitriles
CH513181A (de) * 1969-06-12 1971-09-30 Hoffmann La Roche Verfahren zur Herstellung von N-Oxyden von Benzylpyrimidinen
US3996356A (en) * 1969-07-02 1976-12-07 Hoffmann-La Roche Inc. Composition containing 5-sulfanilamido-3,4-dimethylisoxazole and a trimethoxybenzyl pyrimidine
US3692787A (en) * 1970-02-16 1972-09-19 Burroughs Wellcome Co Substituted 2,4-diamino-5-benzyl pyrimidines
US3684810A (en) * 1970-03-11 1972-08-15 Hoffmann La Roche Process for 2,4-diamino-5-(3,5-dimethoxy-4-hydroxybenzyl) pyrimidine
US3993761A (en) * 1971-12-01 1976-11-23 Hoffmann-La Roche Inc. Antibacterial compositions
BE792096A (fr) * 1971-12-01 1973-05-30 Hoffmann La Roche Nouvelles benzylpyrimidines
BE795023A (fr) * 1972-02-07 1973-08-06 Hoffmann La Roche Nouvelles benzylpyrimidines
IT1044231B (it) * 1972-03-16 1980-03-20 Hoffmann La Roche Combinazione di sostanze attive utile per combattere infezioni da batteri gram positivi e gran negativi
DE2342213C3 (de) * 1972-10-12 1979-10-18 F. Hoffmann-La Roche & Co Ag, Basel (Schweiz) Verwendung von potenzierten SuIf onamiden bei der Behandlung oder Verhinderung von Fischinfektionen
ZA738760B (en) * 1972-12-21 1974-08-28 Hoffmann La Roche Process for the manufacture of benzyl pyrimidines
US4143227A (en) * 1973-02-26 1979-03-06 Hoffmann-La Roche Inc. Process for substituted 5-benzyl-2,4-diamino-pyrimidines
US3931181A (en) * 1973-07-27 1976-01-06 Hoffmann-La Roche Inc. 2,4-Diamino-5-benzylpyrimidines
CH591456A5 (ru) * 1973-09-12 1977-09-15 Hoffmann La Roche
JPS6119628B2 (ru) * 1973-11-08 1986-05-17 Efu Hofuman Ra Roshu Unto Co Ag
US4076810A (en) * 1973-11-08 1978-02-28 Hoffmann-La Roche Inc. Benzylpyrimidine antibacterial composition
CH591457A5 (ru) * 1973-11-08 1977-09-15 Hoffmann La Roche
US4033962A (en) * 1975-06-26 1977-07-05 Hoffman-La Roche Inc. 2,4-Diamino-pyrimidine derivatives and processes
NL7609171A (nl) * 1975-08-29 1977-03-02 Hoffmann La Roche Werkwijze voor het bereiden van antibacte- riele middelen.
GB1582245A (en) * 1976-06-09 1981-01-07 Wellcome Found Benzyl cyanoacetal derivatives and their conversion to pyrimidine derivatives
DE2635765C3 (de) * 1976-08-09 1979-02-08 Ludwig Heumann & Co Gmbh, 8500 Nuernberg Verfahren zur Herstellung von 2,4-EMamino-5-(3',4'r5'-trimethoxybenzyl)-pyrimidin
LU77364A1 (ru) * 1977-05-18 1979-01-19
JPS55102517A (en) * 1979-01-30 1980-08-05 Shionogi & Co Ltd Preparation of sulfamethoxazole-trimethoprim complex for administration via body cavity
DE2944145A1 (de) * 1979-11-02 1981-05-14 Dynamit Nobel Ag, 5210 Troisdorf Verfahren zur herstellung von 2,4-diaminopyrimidin
JPS57109713A (en) * 1980-12-26 1982-07-08 Shionogi & Co Ltd Pharmaceutical preparation of combined agent of sulfamethoxazole and trimethoprim for medication through celom
IT1138146B (it) * 1981-08-11 1986-09-17 Proter Spa Processo per la produzione della 2,4-diammino-(3,5-dimetossi-4-metos sietossi-benzil)-pirimidina
FI64427C (fi) * 1982-05-13 1989-11-08 Uponor Nv Lattiakaivo tai muu kuppimainen vesilukko.
HU197670B (en) * 1986-02-28 1989-05-29 Egyt Gyogyszervegyeszeti Gyar Process for producing composition comprising 2,4-diamino-5-(3,4-dimethoxybenzyl)-pyrimidine or pharmaceutically suitable acid addition salt thereof as active ingredient
FR2595697B1 (fr) * 1986-03-13 1988-07-08 Rousselot Cie Derives de benzyl-pyrimidine, leur procede de preparation ainsi que les compositions en contenant
US4857651A (en) * 1987-07-29 1989-08-15 American Cyanamid Company α-(2,3-Di(C1 -C4 alkoxy)ethylamino)-β-cyanostyrene and β-nitrostyrene compounds useful as intermediates in the preparation of insecticidal, acaricidal and nematicidal arylpyrroles and method for the preparation thereof
US4996198A (en) * 1988-07-11 1991-02-26 Hoffmann-La Roche Inc. Anticoccidial composition
US5135924A (en) * 1989-01-03 1992-08-04 Hoffmann-La Roche Inc. Therapeutic treatment of animals with oral administration of ormetoprim-potentiated sulfonamides
US5158979A (en) * 1989-04-19 1992-10-27 New York University Method and compositions for treating pneumocystic carini infections
US5258373A (en) * 1991-07-17 1993-11-02 Hoffmann-La Roche Inc. Anticoccidial compositions
DE4333688C2 (de) * 1993-10-02 2003-11-06 Guenter Ege Verfahren zur Herstellung von 3-Aryl-2-(dialkoxymethyl)-propannitrilen und ihre Umsetzung zu 5-Arylmethyl-2,4-diamino-pyrimidinen, insbesondere zu Trimethoprim
US5514681A (en) * 1994-08-17 1996-05-07 Virginia Tech Intellectual Properties, Inc. Compositions and methods for controlling pest insects
TW438796B (en) * 1996-05-15 2001-06-07 Hoffmann La Roche 2,4-diaminopyrimidine derivatives, the manufacture process thereof, and the antibiotically-active pharmaceutical composition containing the same
US20090162858A1 (en) * 2007-09-18 2009-06-25 Cornish Virginia W Orthogonal chemical inducer of dimerization
CA2703261C (en) * 2007-10-29 2013-10-08 Nippon Suisan Kaisha, Ltd. Antiparasitic agent for fish and method of controlling proliferation of fish parasites
TWI429397B (zh) * 2009-04-27 2014-03-11 Nippon Suisan Kaisha Ltd 含有葉酸合成抑制劑及/或葉酸活性化抑制劑之組成物的用途
FR3049861A1 (fr) 2016-04-07 2017-10-13 Univ Claude Bernard Lyon Nouvelles compositions antivirales pour le traitement de la grippe
CN106083653A (zh) * 2016-06-06 2016-11-09 江苏天和制药有限公司 奥美普林中间体肉桂腈的合成方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2628236A (en) * 1953-02-10 S-benzyl
US3049544A (en) * 1962-08-14 Method for the preparation of
US2658897A (en) * 1951-06-27 1953-11-10 Burroughs Wellcome Co 2, 4-diamino-5-benzyl pyrimidines
GB734801A (en) * 1953-03-06 1955-08-10 Wellcome Found Improvements in and relating to derivatives of pyrimidine and the manufacture thereof
US2783178A (en) * 1954-06-22 1957-02-26 American Scient Lab Inc Stable concentrated sulfaquinoxaline solutions and method for preparing
US2823160A (en) * 1955-03-29 1958-02-11 Whitmoyer Lab Inc Substituted pyrimidines compositions for chemotherapy of coccidiosis
US2909522A (en) * 1957-02-21 1959-10-20 Burroughs Wellcome Co Trialkoxybenzylpyrimidines and method
DE1303727B (de) * 1959-09-03 1976-02-05 Ausscheidung aus: 14 45 176 The Wellcome Foundation Ltd., London Alpha-Arylidensubstituierte Propioni-Irile
US3085937A (en) * 1960-11-21 1963-04-16 Shionogi & Co Method of combating coccidiosis with sulfonamide compositions
US3485840A (en) * 1964-11-12 1969-12-23 Hoffmann La Roche 2,4-diamino - 5 - (2',4',5'-substituted benzyl) pyrimidines,intermediates and processes

Also Published As

Publication number Publication date
NL6514472A (ru) 1966-05-13
DK115847B (da) 1969-11-17
GB1132086A (en) 1968-10-30
GB1132083A (en) 1968-10-30
SE326185B (ru) 1970-07-20
IL24534A (en) 1969-12-31
CH467270A (de) 1969-01-15
BE671981A (ru) 1966-05-09
DE1545967C3 (de) 1974-12-19
IL24497A (en) 1969-11-12
GB1132085A (en) 1968-10-30
IL32695A (en) 1969-12-31
GB1132082A (en) 1968-10-30
US3485840A (en) 1969-12-23
GB1062508A (en) 1967-03-22
NL6514178A (ru) 1966-05-13
US3461206A (en) 1969-08-12
DE1545967A1 (de) 1969-11-20
BR6574667D0 (pt) 1973-08-16
BE671982A (ru) 1966-05-09
NL6514743A (ru) 1966-05-13
SE311160B (ru) 1969-06-02
NO115741B (ru) 1968-11-25
MY7200071A (en) 1972-12-31
GB1132084A (en) 1968-10-30
US3341541A (en) 1967-09-12
NL163213C (nl) 1980-08-15
FR5411M (ru) 1967-10-02
IL32696A (en) 1969-12-31
DE1545967B2 (de) 1974-05-16
CH467784A (de) 1969-01-31
GB1133766A (en) 1968-11-20
BR6574670D0 (pt) 1973-08-07
IL24498A (en) 1969-07-30
FI43251B (ru) 1970-11-02
IL32694A (en) 1969-12-31
BE671983A (ru) 1966-05-09
SE346314B (ru) 1972-07-03
IL32697A (en) 1969-12-31
NL163213B (nl) 1980-03-17
DE1545966A1 (de) 1970-02-26
MY6700159A (en) 1967-12-31
IT1058251B (it) 1982-04-10
SE327122B (ru) 1970-08-10
BR6574668D0 (pt) 1973-08-07
NO119948B (ru) 1970-08-03

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