Method for preparing 2-[n-(1-adamantyl)benzyl]thio-6-methylpyrimidin-4(3h)-one

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for synthesis of 2-[n-(1-adamantyl)benzyl]thio-6-methylpyrimidin-4(3H)-one of the formula: that can be used as a semiproduct in synthesis of medicinal preparations. Method involves dissolving 6-methyl-2-thiouracil in sodium hydroxide an aqueous solution in the mole ratio 6-methyl-2-thiouracil : sodium hydroxide = 1:1.1 to yield 6-methyl-2-thiouracil S-sodium salt that is subjected for interaction with n-(1-adamantyl)benzyl bromide in the mole ratio = 1:1.1, respectively, at temperature 30-50°C for 15-30 min in dioxane medium, Method provides preparing indicated compound with the high yield.

EFFECT: improved method of synthesis.

3 ex

 

The present invention relates to the field of synthesis of heterocyclic compounds specifically to a method for producing 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-it formula

which can be used as an intermediate in the synthesis of pharmaceuticals.

A method of obtaining substances similar in structure, S-derivatives of 2-thiouracil reaction of different 5,6-substituted 2-thiouracil with benzyl(pyridinyl)bromide in ethanol medium at the boiling temperature of the solvent for one and a half hours leads to the production of S-benzyl(pyridinyl)derivatives of 5,6-substituted 2-thiouracil. (U.S. Pat. 5981537 USA, IPC6A 61 K 31/505, C 07 D 413/00. Pyrimidine-thioalkyl and alkylether compounds / Pharmacia and Upion Co., Nugent Richard F., Schlachther Stephen T., Pa. - 1999)

A method of obtaining S-derivatives of 2-thiouracil of 6-methyl-2-thiouracil in the environment of N,N-dimethylformamide in the presence of K2CO3at a temperature of 75-80° (Novikov, M. R., A. Ozerov, Brel A.K., Navrotsky, M. B., SIM OG Chemistry and technology of Organoelement monomers and polymeric materials: collected scientific articles. Works / VSTU. - Volgograd, 2002. - P.53-56).

These methods have significant drawbacks. First, these methods do not provide a high yield of reaction products (46-73%), and second, the prolonged heating of the reaction mixture at a sufficiently high is their temperatures.

The connection of the proposed structure in the literature and patent sources not found.

The objective of the proposed technical solution is to develop a technologically advanced method of obtaining 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-it allows to carry out the synthesis under mild conditions using cheap raw materials and to obtain 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-he almost quantitative yield.

The technical result is to obtain a new connection with practically quantitative yield.

This technical result is achieved in a method of producing 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-it formula

consisting in dissolving 6-methyl-2-thiouracil in aqueous caustic soda solution at a molar ratio of 6-methyl-2-thiouracil:caustic soda to 1:1.1 with getting S-sodium salt of 6-methyl-2-thiouracil, which is subjected to interaction with n-(1-substituted)benzylbromide at a molar ratio of 1:1.1, respectively, at a temperature of 30-50°C for 15-30 min in an environment of dioxane.

The essence of the proposed method is a nucleophilic substitution of the halogen atom in the n-(1-substituted)benzylbromide anion of 2-thiouracil, with the formation of the target product with practically quantitative yield (91-97%).

The use of caustic soda in the proposed process, it is necessary to convert the original 6-methyl-2-thiouracil in the water-soluble sodium salt. These temperature intervals and duration of the reaction is selected, based on the fact that at a temperature of less than 30°With time and the reaction of 15 min, the required yield of 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-she is not reached and if the temperature is above 50°With time and carrying out the reaction over 30 min, the increase in output is not observed. The proposed method differs in that environment dioxane from the S-sodium salt of 6-methyl-2-thiouracil is generated anion 2-thiouracil. When choosing a solvent for the reaction of 6-methyl-2-thiouracil with n-(1-substituted)benzylbromide we have taken into account the following requirements: create a homogeneous reaction mixture, maintaining the desired temperature and the polarity of the solvent. All these requirements are met dioxane, it dissolves all reagents, it is possible to maintain the temperature of 30-50°and it is sufficiently polar to its environment was used to generate the anion of 2-thiouracil.

The proposed method is as follows.

In an aqueous solution of caustic soda dissolved 6-methyl-2-thiouracil at a molar ratio of 6-methyl-2-thiouracil : caustic soda to 1:1.1 with getting S-sodium salt methyl-2-thiouracil, which is subjected to interaction with n-(1-substituted)benzylbromide at a molar ratio of 1:1.1, respectively, in the environment of dioxane at a temperature of 30-50°C for 15-30 minutes

The invention is illustrated by the following examples.

Synthesis of 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-it.

Example 1.

In 7 ml of water dissolving 0.46 g (11.6 mmol) of sodium hydroxide and 1.5 g (10.6 mmol) of 6-methyl-2-thiouracil. To the solution was added 7 ml of dioxane and added dropwise a solution of 1.45 g (11.6 mmol) of n-(1-substituted)benzylbromide in 4.2 ml of dioxane. The molar ratio of caustic soda: 6-methyl-2-thiouracil, n-(1-substituted)benzylbromide 1.1:1.0:1.1, respectively. The mixture is stirred for 15 min at 50°C. After cooling, the precipitated precipitate is filtered off, washed with cold water, dried and recrystallized from benzene. The yield of 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-it 2.5 g (97%), white crystals, TPL 162-164°C. the Spectrum of TMR, δ, M. D.: 1.65-1.8 m (15 N, Adamantine); s (3 H, CH3); S (2 H, SCH2); 5. S (1H, H-5); 7.2-7.4 m (4H, aromatic); 12.5 (1H, NH).

Example 2.

In 7 ml of water dissolving 0.46 g (11.6 mmol) of sodium hydroxide and 1.5 g (10.6 mmol) of 6-methyl-2-thiouracil. To the solution was added 7 ml of dioxane and added dropwise a solution of 1.45 g (11.6 mmol) of n-(1-substituted)benzylbromide in 4.2 ml of dioxane. The molar ratio of caustic soda: 6-methyl-2-thiouracil, n-(1-substituted)benzylbromide 1.1:1.0:1.1, respectively. The mixture premesis the Ute 20 min at 40° C. After cooling, the precipitated precipitate is filtered off, washed with cold water, dried and recrystallized from benzene. The yield of 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-she 2.4 g (94%).

Example 3.

In 7 ml of water dissolving 0.46 g (11.6 mmol) of sodium hydroxide and 1.5 g (10.6 mmol) of 6-methyl-2-thiouracil. To the solution was added 7 ml of dioxane and added dropwise a solution of 1.45 g (11.6 mmol) of n-(1-substituted)benzylbromide in 4.2 ml of dioxane. The molar ratio of caustic soda : 6-methyl-2-thiouracil, n-(1-substituted)benzylbromide 1.1:1.0:1.1, respectively. The mixture is stirred for 30 min at 30°C. After cooling, the precipitated precipitate is filtered off, washed with cold water, dried and recrystallized from benzene. The yield of 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-she 2.35 g (91%).

It follows from the presented examples, we proposed a method of obtaining 2-(n-(1-substituted)thio-6-methylpyrimidin-4(3H)-it is a technology that allows to obtain the specified connection with practically quantitative yield.

The method of obtaining 2-(n-(1-substituted)benzyl)thio-6-methylpyrimidin-4(3H)-it formula

consisting in dissolving 6-methyl-2-thiouracil in aqueous caustic soda solution at a molar ratio of 6-methyl-2-thiouracil: caustic soda 1:1,1 obtaining S-sodium salt of 6-methyl-2-thiouracil, which is subjected to interaction with n-(1-Adam is ntil)benzylbromide at a molar ratio of 1:1,1 respectively at a temperature of 30-50° C for 15-30 min in an environment of dioxane.



 

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< / BR>
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