GB1128234A

GB1128234A – 5-benzylpyrimidine derivatives and process for the preparation thereof
– Google Patents

GB1128234A – 5-benzylpyrimidine derivatives and process for the preparation thereof
– Google Patents
5-benzylpyrimidine derivatives and process for the preparation thereof

Info

Publication number
GB1128234A

GB1128234A
GB737666A
GB737666A
GB1128234A
GB 1128234 A
GB1128234 A
GB 1128234A
GB 737666 A
GB737666 A
GB 737666A
GB 737666 A
GB737666 A
GB 737666A
GB 1128234 A
GB1128234 A
GB 1128234A
Authority
GB
United Kingdom
Prior art keywords
group
benzyl
hydrogen
halogen
hydrogen atom
Prior art date
1966-02-19
Legal status (The legal status 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 status listed.)

Expired

Application number
GB737666A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Wellcome Foundation Ltd

Original Assignee
Wellcome Foundation Ltd
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.)
1966-02-19
Filing date
1966-02-19
Publication date
1968-09-25

1966-02-19
Application filed by Wellcome Foundation Ltd
filed
Critical
Wellcome Foundation Ltd

1966-02-19
Priority to GB737666A
priority
Critical
patent/GB1128234A/en

1967-02-13
Priority to IL2742467A
priority
patent/IL27424A/en

1967-02-13
Priority to GR670133641A
priority
patent/GR33641B/en

1967-02-15
Priority to CA983,015A
priority
patent/CA977754A/en

1967-02-16
Priority to AT409368A
priority
patent/AT275534B/en

1967-02-16
Priority to NO16687667A
priority
patent/NO124601B/no

1967-02-16
Priority to AT153867A
priority
patent/AT270653B/en

1967-02-17
Priority to DE1967W0043385
priority
patent/DE1720012B2/en

1967-02-17
Priority to DE19671795635
priority
patent/DE1795635C3/en

1967-02-17
Priority to FI48067A
priority
patent/FI49714C/en

1967-02-17
Priority to BE694244D
priority
patent/BE694244A/xx

1967-02-17
Priority to CH191468A
priority
patent/CH513179A/en

1967-02-17
Priority to CH237967A
priority
patent/CH511239A/en

1967-02-17
Priority to NL6702397A
priority
patent/NL146811B/en

1967-02-17
Priority to ES336945A
priority
patent/ES336945A1/en

1967-02-20
Priority to SE796270A
priority
patent/SE390412B/en

1967-02-20
Priority to SE227867A
priority
patent/SE338998B/xx

1967-02-20
Priority to DK91167A
priority
patent/DK120344B/en

1967-02-20
Priority to FR95595A
priority
patent/FR1536204A/en

1967-05-16
Priority to FR106573M
priority
patent/FR6595M/fr

1968-02-02
Priority to FI26868A
priority
patent/FI55031C/en

1968-02-02
Priority to FR138498A
priority
patent/FR94837E/en

1968-02-02
Priority to DE19681720031
priority
patent/DE1720031A1/en

1968-09-25
Publication of GB1128234A
publication
Critical
patent/GB1128234A/en

1971-02-10
Priority to DK59371A
priority
patent/DK128247B/en

1971-09-07
Priority to FI250271A
priority
patent/FI55032C/en

1971-10-13
Priority to NO377771A
priority
patent/NO133550C/no

1971-12-31
Priority to MY7100226A
priority
patent/MY7100226A/en

Status
Expired
legal-status
Critical
Current

Links

Espacenet

Global Dossier

Discuss

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

C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine

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

C07D239/50—Three nitrogen atoms

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

Abstract

1,128,234. 5-Benzyl-pyrimidine derivatives. WELLCOME FOUNDATION Ltd. (Burroughs Wellcome & Co. (U.S.A.) Inc.). 16 Feb., 1967 [19 Feb., 1966], No. 7376/66. Heading C2C. 5-Benzyl-pyrimidine derivatives of the formula wherein X and Y are the same or different and each is an amino or hydroxyl group, Z is a hydrogen atom, an alkyl group containing not more than 4 carbon atoms, an hydroxyl group, or a substituted or unsubstituted amino group, the said substituted amino group including a cyclic amino group, such as a piperidino or morpholino group, R1 is a hydrogen atom or a saturated or unsaturated hydrocarbon radical which may be optionally substituted by halogen, and R2 and R3 are the same or different and each is a hydrogen atom, a halogen atom, or an alkyl or alkoxy group containing not more than 4 carbon atoms, are prepared by reacting together a pyrimidine derivative and a Mannich base of the respective formulµ wherein NR 2 4 is a dialkylamino or a cyclicamino group, and optionally reacting the resulting novel 5-benzyl-pyrimidine derivative of the first formula above wherein R1 is hydrogen with a compound R1Q, wherein Q is a reactive atom or group and R1 is a saturated or unsaturated hydrocarbon radical which may be optionally substituted by halogen, under basic conditions. 2,6 – Dimethoxy – 4 – (N,N – dimethylaminomethyl)-phenol is prepared by reacting together 2,6-dimethoxyphenol, dimethylamine and formaldehyde. Pharmaceutical compositions having antibacterial activity comprise as active ingredient a 5-benzyl-pyrimidine derivative of the first formula above wherein R1 is hydrogen in admixture with a pharm aceutically acceptable carrier.

GB737666A
1966-02-19
1966-02-19
5-benzylpyrimidine derivatives and process for the preparation thereof

Expired

GB1128234A
(en)

Priority Applications (27)

Application Number
Priority Date
Filing Date
Title

GB737666A

GB1128234A
(en)

1966-02-19
1966-02-19
5-benzylpyrimidine derivatives and process for the preparation thereof

IL2742467A

IL27424A
(en)

1966-02-19
1967-02-13
Method of preparing 5-benzylpyrimidines and novel 5-benzylpyrimidines

GR670133641A

GR33641B
(en)

1966-02-19
1967-02-13

CHEMICAL COMPOSITIONS AND METHOD.

CA983,015A

CA977754A
(en)

1966-02-19
1967-02-15
2-(3′,4′,5′-trisubstituted-benzyl) pyrimidine compounds

AT409368A

AT275534B
(en)

1966-02-19
1967-02-16

Process for the preparation of 5-benzylpyrimidines

NO16687667A

NO124601B
(en)

1966-02-19
1967-02-16

AT153867A

AT270653B
(en)

1966-02-19
1967-02-16

Process for the preparation of new 5-benzylpyrimidines

NL6702397A

NL146811B
(en)

1966-02-19
1967-02-17

PROCESS FOR THE PREPARATION OF 5-BENZYLPYRIMIDINE DERIVATIVES.

DE19671795635

DE1795635C3
(en)

1966-02-19
1967-02-17

2,4-diamino-5-benzyl pyrimidines

FI48067A

FI49714C
(en)

1966-02-19
1967-02-17

Process for the preparation of 5-benzylpyrimidines.

BE694244D

BE694244A
(en)

1966-02-19
1967-02-17

CH191468A

CH513179A
(en)

1966-02-19
1967-02-17

Process for the preparation of 5-benzylpyrimidines

CH237967A

CH511239A
(en)

1966-02-19
1967-02-17
Antibacterial benzylpyrimidines

DE1967W0043385

DE1720012B2
(en)

1966-02-19
1967-02-17

Process for the preparation of 2,4-DIAMINO-5- (3,4,5-TRIMETHOXYBENZYL) -PYRIMIDINE

ES336945A

ES336945A1
(en)

1966-02-19
1967-02-17
5-benzylpyrimidine derivatives and process for the preparation thereof

FR95595A

FR1536204A
(en)

1966-02-19
1967-02-20

Process for the preparation of pyrimidine derivatives

SE227867A

SE338998B
(en)

1966-02-19
1967-02-20

DK91167A

DK120344B
(en)

1966-02-19
1967-02-20

Process for the preparation of 5-benzyl-pyrimidines.

SE796270A

SE390412B
(en)

1966-02-19
1967-02-20

2,4-DIAMINO-5- (4′-HYDROXYBENZYL) PYRIMIDINES FOR USE, AS A STARTING MATERIAL FOR THE PREPARATION OF 2,4-DIAMINO-5- (3 ‘, 4′, 5′-TRIALICOCIBENSYL) PYRIMIDINES

FR106573M

FR6595M
(en)

1966-02-19
1967-05-16

DE19681720031

DE1720031A1
(en)

1966-02-19
1968-02-02

Biologically active 5-benzylpyrimidine derivatives and processes for their preparation

FR138498A

FR94837E
(en)

1966-02-19
1968-02-02

Process for the preparation of pyrimidine derivatives.

FI26868A

FI55031C
(en)

1966-02-19
1968-02-02

FREQUENCY REFRIGERATION OF ANTIBACTERIAL 5-BENZYLPYRIMIDINER

DK59371A

DK128247B
(en)

1966-02-19
1971-02-10

2,4-Diamino-5- (4’-hydroxybenzyl) -pyrimidines for use as starting materials in the preparation of corresponding compounds in which the hydrogen atom of the hydroxy group is substituted.

FI250271A

FI55032C
(en)

1966-02-19
1971-09-07

SOM UTGAONGSMATERIAL VID FRAMSTAELLNING AV ANTIBAKTERIELLA 2,4-DIAMINO-5- (3 ‘, 4′, 5′-TRIALKOXIBENYL) -PYRIMIDINER ANVAENDBARA 2,4-DIAMINO-5- (4’-HYDROXIBENYL) -PYRIMIDINER

NO377771A

NO133550C
(en)

1966-02-19
1971-10-13

MY7100226A

MY7100226A
(en)

1966-02-19
1971-12-31
5-benzylpyrimidine derivatives and process for the preparation thereof

Applications Claiming Priority (1)

Application Number
Priority Date
Filing Date
Title

GB737666A

GB1128234A
(en)

1966-02-19
1966-02-19
5-benzylpyrimidine derivatives and process for the preparation thereof

Publications (1)

Publication Number
Publication Date

GB1128234A
true

GB1128234A
(en)

1968-09-25

Family
ID=9831956
Family Applications (1)

Application Number
Title
Priority Date
Filing Date

GB737666A
Expired

GB1128234A
(en)

1966-02-19
1966-02-19
5-benzylpyrimidine derivatives and process for the preparation thereof

Country Status (16)

Country
Link

AT
(2)

AT275534B
(en)

BE
(1)

BE694244A
(en)

CA
(1)

CA977754A
(en)

CH
(2)

CH511239A
(en)

DE
(2)

DE1795635C3
(en)

DK
(2)

DK120344B
(en)

ES
(1)

ES336945A1
(en)

FI
(1)

FI49714C
(en)

FR
(1)

FR6595M
(en)

GB
(1)

GB1128234A
(en)

GR
(1)

GR33641B
(en)

IL
(1)

IL27424A
(en)

MY
(1)

MY7100226A
(en)

NL
(1)

NL146811B
(en)

NO
(1)

NO124601B
(en)

SE
(2)

SE390412B
(en)

Cited By (3)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

DE2249532A1
(en)

*

1971-10-12
1973-04-26
Wellcome Found

PROCESS FOR THE PREPARATION OF 2,4-DIAMINO-5-BENZYLPYRIMIDINES

EP0006987A1
(en)

*

1978-05-24
1980-01-23
The Wellcome Foundation Limited
2,4-Diamino-5-benzylpyrimidines, especially for the treatment of microbial infections, pharmaceutical compositions containing these compounds and processes for preparing these compounds

DE2944145A1
(en)

1979-11-02
1981-05-14
Dynamit Nobel Ag, 5210 Troisdorf

METHOD FOR PRODUCING 2,4-DIAMINOPYRIMIDINE

1966

1966-02-19
GB
GB737666A
patent/GB1128234A/en
not_active
Expired

1967

1967-02-13
IL
IL2742467A
patent/IL27424A/en
unknown

1967-02-13
GR
GR670133641A
patent/GR33641B/en
unknown

1967-02-15
CA
CA983,015A
patent/CA977754A/en
not_active
Expired

1967-02-16
AT
AT409368A
patent/AT275534B/en
active

1967-02-16
NO
NO16687667A
patent/NO124601B/no
unknown

1967-02-16
AT
AT153867A
patent/AT270653B/en
active

1967-02-17
ES
ES336945A
patent/ES336945A1/en
not_active
Expired

1967-02-17
NL
NL6702397A
patent/NL146811B/en
not_active
IP Right Cessation

1967-02-17
DE
DE19671795635
patent/DE1795635C3/en
not_active
Expired

1967-02-17
BE
BE694244D
patent/BE694244A/xx
not_active
IP Right Cessation

1967-02-17
DE
DE1967W0043385
patent/DE1720012B2/en
active
Granted

1967-02-17
CH
CH237967A
patent/CH511239A/en
not_active
IP Right Cessation

1967-02-17
CH
CH191468A
patent/CH513179A/en
not_active
IP Right Cessation

1967-02-17
FI
FI48067A
patent/FI49714C/en
active

1967-02-20
SE
SE796270A
patent/SE390412B/en
unknown

1967-02-20
DK
DK91167A
patent/DK120344B/en
not_active
IP Right Cessation

1967-02-20
SE
SE227867A
patent/SE338998B/xx
unknown

1967-05-16
FR
FR106573M
patent/FR6595M/fr
not_active
Expired

1971

1971-02-10
DK
DK59371A
patent/DK128247B/en
not_active
IP Right Cessation

1971-12-31
MY
MY7100226A
patent/MY7100226A/en
unknown

Cited By (3)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

DE2249532A1
(en)

*

1971-10-12
1973-04-26
Wellcome Found

PROCESS FOR THE PREPARATION OF 2,4-DIAMINO-5-BENZYLPYRIMIDINES

EP0006987A1
(en)

*

1978-05-24
1980-01-23
The Wellcome Foundation Limited
2,4-Diamino-5-benzylpyrimidines, especially for the treatment of microbial infections, pharmaceutical compositions containing these compounds and processes for preparing these compounds

DE2944145A1
(en)

1979-11-02
1981-05-14
Dynamit Nobel Ag, 5210 Troisdorf

METHOD FOR PRODUCING 2,4-DIAMINOPYRIMIDINE

Also Published As

Publication number
Publication date

CH511239A
(en)

1971-08-15

SE338998B
(en)

1971-09-27

AT275534B
(en)

1969-10-27

DE1795635A1
(en)

1972-10-19

FI49714C
(en)

1975-09-10

SE390412B
(en)

1976-12-20

DK128247B
(en)

1974-03-25

AT270653B
(en)

1969-05-12

NL146811B
(en)

1975-08-15

DK120344B
(en)

1971-05-17

IL27424A
(en)

1971-02-25

MY7100226A
(en)

1971-12-31

CH513179A
(en)

1971-09-30

FR6595M
(en)

1969-01-06

DE1720012A1
(en)

1972-04-06

GR33641B
(en)

1968-01-03

BE694244A
(en)

1967-08-17

DE1795635B2
(en)

1977-09-22

DE1795635C3
(en)

1978-05-11

NO124601B
(en)

1972-05-08

FI49714B
(en)

1975-06-02

DE1720012B2
(en)

1977-06-08

NL6702397A
(en)

1967-08-21

CA977754A
(en)

1975-11-11

ES336945A1
(en)

1968-01-16

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