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A solution of <strong>[57808-65-8]closantel</strong> in a mixed solvent system of acetonitrile and tetrahydrofuran is treated with an equimolar amount of monoisopropanolamine. The reaction is stirred at 40 C, and then room temperature. Evapoaration of the solvents leads to the isolation of the monoisopropanolamine salt of <strong>[57808-65-8]closantel</strong>. After purification using the standard methods, the salt is characterized.
N-methylglucamine is added to a suspension of <strong>[57808-65-8]closantel</strong> in ethanol, benzyl alcohol, and propylene glycol. With stirring, the salt of <strong>[57808-65-8]closantel</strong> forms in situ, forming a solution. Moxidectin is then added, and stirred until solution is obtained. The formulation is then brought to volume with propylene glycol.
Diethanolamine is added to a suspension of <strong>[57808-65-8]closantel</strong> in ethanol, benzyl alcohol, and propylene glycol. With stirring, the salt of <strong>[57808-65-8]closantel</strong> forms in situ, forming a solution. Moxidectin is then added, and stirred until solution is obtained. The formulation is then brought to volume with propylene glycol.
EXAMPLE 1 Preparation Of A Pour-On Formulation Containing An Organic Amine Salt Of <strong>[57808-65-8]Closantel</strong> Ingredients g/200 mL % w/v <strong>[57808-65-8]Closantel</strong> 60.00 30.00 Diethylene glycol 60.0 30.00 Monoethyl ether Ethanol amine 6.6 3.30 Benzyl alcohol 10.0 5.00 Oleic acid 60.0 30.00 Moxidectin 1.04 0.52 Ethanol, USP qs to 200 ml qs to 100 A stirred mixture of <strong>[57808-65-8]closantel</strong> in diethylene glycol monoethyl ether is treated with ethanolamine, and stirring is continued until solution is complete, thus forming the salt in situ. To this solution is then added a solution of moxidectin in benzyl alcohol, followed by the addition of oleic acid and ethanol. Stirring is continued until the mixture is homogeneous.
In 2-pyrrolidinon; polypropylene glycol 400; benzyl alcohol;
Ethanolamine is added to a suspension of <strong>[57808-65-8]closantel</strong> in benzyl alcohol, 2- pyrrolidone and polypropylene glycol 400. With stirring, the salt of formed in situ, forming a solution. Moxidectin is then added, and stirred until solution is obtained. The formulation is then brought to volume with PEG 400.
A solution of <strong>[57808-65-8]closantel</strong> in a mixed solvent system of acetonitrile and tetrahydrofuran is treated with an equimolar amount of diisopropanolamine. The reaction is stirred at 40 C, and then room temperature. Evaporation of the solvents leads to the isolation of the diisopropanolamine salt of <strong>[57808-65-8]closantel</strong>. After purification using the standard methods, the salt is characterized.
EXAMPLE XXXII A warm solution of 1 part of N-{5-chloro-4-[alpha-(4-chlorophenyl)-alpha-cyanomethyl]-2-methylphenyl}-2-hydroxy-3,5-diiodobenzamide, 0.3 parts of sodium hydroxide solution 10N, 8 parts of methanol and 10 parts of water is allowed to crystallize. The product is filtered off, washed with water and dried, yielding 0.7 parts (67.5%)of N-{5-chloro-4-[alpha-(4-chlorophenyl)-alpha-cyanomethyl]-2-methylphenyl}-2-hydroxy-3,5-diiodobenzamide, sodium salt hydrate; mp. 270 -300 C.
7
[ 123-91-1 ]
[ 42016-91-1 ]
[ 61437-85-2 ]
[ 57808-65-8 ]
Yield
Reaction Conditions
Operation in experiment
EXAMPLE X A mixture of 4 parts of 2-hydroxy-3,5-diiodobenzoyl chloride, 2.9 parts of 4-amino-2-chloro-alpha-(4-chlorophenyl)-5-methylbenzeneacetonitrile and 75 parts of 1,4-dioxane is stirred and refluxed for 10 minutes. The reaction mixture is evaporated and the oily residue is crystallized from methanol. The product is filtered off and dried, yielding 5.3 parts of N-{5-chloro-4-[alpha-(4-chlorophenyl)-alpha-cyanomethyl]-2-methylphenyl}-2-hydroxy-3,5-diiodobenzamide; mp. 217.8 C.
With sodium hydroxide; In water; at 70.0℃; for 6.0h;Sealed tube;
In a 1000 mL sealed four-neck reaction flask, 80 g of sodium hydroxide and 500 mL of water were added and stirred uniformly and was added to the above obtained Example 7 663.1 g of <strong>[57808-65-8]closantel</strong> (IV), and the mixture was heated to 70 C for 6 hours. After cooling to room temperature and filtration, a pale yellow solid <strong>[57808-65-8]closantel</strong> sodium (I) 680.3 g was obtained, yield 99.3%.
In toluene; at 50.0℃; for 6.0h;Reflux; Sealed tube;
In a 1000 mL sealed four-neck reaction flask, 291.2 g of 4-amino-2-chloro-5-methyl-alpha-(4-chlorophenyl)phenylacetonitrile (III) and 500 mL of toluene were added, stirred and dissolved, and the temperature was controlled at 50C, 389.9 g of 2-hydroxy-3,5-diiodobenzoyl chloride in toluene solution was added dropwise, and the dropwise addition time was 1 hour. After the completion of the dropwise addition, the temperature was raised to reflux and stirring was continued for 5 hours.After completion of the reaction, the reaction was completed, and the solvent toluene was recovered to give a pale-yellow solid, closantel (IV), 590.8 g, yield: 89.1%.
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