摘要:
The present invention relates to new aminophenylamidines, to processes for their production, and to their pharmaceutical use. These new compounds are useful as paraciticides, especially as anthelmintics. Some acylaminophenylformamidines, such as N-(p-acetamidophenyl)N'',N''-dimethylformamidine (U.S. Pat. No. 3,184,482) and N-phenylacetamidines, such as N-(p-chlorophenyl)-N'',N''dimethylacetamidine, are already known. These compounds are however inactive against the helminths mentioned below.
摘要:
PHOSPHOROUS-CONTAINING A-OXIMINO-ARYL ACETIC ACID NITRILE HAVING THE FORMULA:
R1-O-P(=X)(-R2)-O-N=C(-CN)-R3
IN WHICH R1 IS ALKYL AND HALOALKYL; R2 IS ALKYL ALKOXY, HALOALKOXY, ALKYL AMINO, DI-ALKYL AMINO, PHENYL, PHENOXY, CYCLOHEXYL AND CYCLOHESYLOXY; R3 IS PHEYL, NAPHTHYL, PRYIDYL AND SUBSTITUTED PHENYL WHICH IS SUBSTITUTED WITH MONO-, DI- AND TRIHALO, ALKYL, ALKOXY MERCAPTO AND/ OR NITRO; AND X IS OXYGEN AND SULFUR, WHICH POSSESS BIOCIDAL PROPERTIES, AND WHICH MAY BE PREPARED BY REACTING THE CORRESPONDING PHOSPHORUS ESTER HALIDE WITH THE APPROPRIATE A-OXIMINO ARYLACETIC ACID NITRILE IN THE FORM OF THE CORRESPONDING SALT OR IN THE PRESENCE OF AN ACIDBINDING AGENT. THE COMPOUNDS ARE PESTICIDES.
摘要:
4-Amino substituted phenylamidine are anthelmintics. The compounds, of which N-(4-aminophenyl)-N'',N''-dimethylacetamidine is a representative embodiment, can be prepared through treatment of a 4-amino aniline with a carboxylic acidamide or thioamide, reduction of an appropriately substituted 4-aminophenyl-amidine, optionally followed by alkylation of the resultant 4-aminophenylamidine, formation of a Schiff base followed by quaternization and hydrolysis, or hydrolysis of a 4-acylaminophenylamidine.
摘要:
2-(4-Aminophenylimino) derivatives of thiazolidine and -4H-5,6dihydro-1,3-thiazines, the corresponding amide and sulfonamide derivatives, and the salts thereof are anthelmintic agents. The compounds, of which 2-(4-aminophenylimino)-N-methylthiazolidine is a typical embodiment, are prepared through cyclization of a thiourea, optionally with subsequent hydrolysis, alkylation or acetylation.
摘要:
4-Amino substituted phenylamidine are anthelmintics. The compounds, of which N-(4-aminophenyl)-N'',N''-dimethylacetamidine is a representative embodiment, can be prepared through treatment of a 4-amino aniline with a carboxylic acidamide or thioamide, reduction of an appropriately substituted 4-aminophenylamidine, optionally followed by alkylation of the resultant 4-aminophenylamidine, formation of a Schiff base followed by quaternization and hydrolysis, or hydrolysis of a 4-acylaminophenylamidine.
摘要:
Compositions and methods of using phosphoryl-, phosphonyl-, thionophosphoryl- and thionophosphonyl- - Alpha -oximinoarylacetic acid nitriles which possess pesticidal, especially insecticidal and/or acaricidal, properties, and which may be produced by reacting the corresponding phosphorus acid ester halide with the corresponding Alpha -oximino-arylacetic acid nitrile.
摘要:
Phosphonic and thiphosphonic acid esters of 2-hydroxy 3,5,6-trichloropyridine, R1 = alkyl-R2 = alkyl-, phenyl-X = O or S Insecticides, acaricides. Potassium carbonate is added to a suspension of 2-hydroxy 3,5,6-trichloropyridine in acetonitrile and the mixture warmed to 60 deg. C for 1/2 hour. When the temperature has cooled to 50 deg. C methylthiono-phosphonic O-ethyl chloride is added dropwise. The mixture is heated for 4 hrs. at 70 deg. C and the stirring is continued for another 3 hrs. After filtration of the separated sodium chloride the filtrate is extracted with benzene. The benzene solution is washed with water, dried and the solvent distilled off. Recrystallisation of the residue from ethanol yields O-ethyl O-(3,5,6-trichloropyridyl-2) methylthiono-phosphonate.
摘要:
4-Amino substituted phenylamidine are anthelmintics. The compounds, of which N-(4-aminophenyl)-N'',N''-dimethylacetamidine is a representative embodiment, can be prepared through treatment of a 4-amino aniline with a carboxylic acidamide or thioamide, reduction of an appropriately substituted 4-aminophenylamidine, optionally followed by alkylation of the resultant 4-aminophenylamidine, formation of a Schiff base followed by quaternization and hydrolysis, or hydrolysis of a 4-acylaminophenylamidine.
摘要:
The present invention relates to new aminophenylamidines and cycloamidines and salts thereof, to processes for their production, and to their use as medicines, especially as parasiticides. Acylaminophenylformamidines, such as N-(p-acetamidophenyl)-N'', N''-dimethylformamidine (U.S. Pat. No. 3,184,482) are already known. This compound, as well as other formamidine derivatives, are, however, ineffective against helminths. Furthermore, Nphenylacetamidines, such as N-(p-chlorophenyl)-N'',N''dimethylacetamidine, are known. These compounds are also ineffective against helminths.
摘要:
4-Amino substituted phenylamidine are anthelmintics. The compounds, of which N-(4-aminophenyl)N'',N''-dimethylacetamidine is a representative embodiment, can be prepared through treatment of a 4-amino aniline with a carboxylic acidamide or thioamide, reduction of an appropriately substituted 4-amino-phenylamidine, optionally followed by alkylation of the resultant 4aminophenylamidine, formation of a Schiff base followed by quaternization and hydrolysis, or hydrolysis of a 4acylaminophenylamidine.