Fatty Acid Modified Forms of Glucocorticoids
a technology of glucocorticoids and fatty acids, which is applied in the direction of steroid, medical preparations, organic chemistry, etc., can solve the problems of preventing the realization of the maximum pharmacologic value, preventing the effect of adsorption of adsorption, and causing the same side effects as swallowing drugs
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example 1
Synthesis of the Docosahexaenoic Acid Ester of Budesonide
[0020]A solution of 1.0 gm (3×10−3 moles) of docosahexaenoic acid in methylene chloride (10 mL) was treated with thionyl chloride (0.357 gm, 3×10−3 moles) and two drops of DMF. This solution was heated at 30° C. for two hours. After cooling the solvent and any unreacted thionyl chloride were removed under vacuum. The residue was added dropwise to a solution of budesonide (1.0 gm, 2.3×10−3 moles) in pyridine (10 mL) with stirring and ice cooling. After the addition was complete the reaction mixture was stirred at room temperature for one hour. Water (50 mL) containing 85% phosphoric acid (5 mL) was added and the insoluble material was extracted into diethyl ether (50 mL). After discarding the aqueous phase, the ether solution was washed with water (50 mL) containing 85% phosphoric acid (5 mL). The ether solution was dried over magnesium sulfate, then filtered and stripped under vacuum. The residue was purified by chromatography...
example 2
Synthesis of the Docosapentaenoic Acid Ester of Budesonide
[0021]A solution of 1.0 gm (3×10−3 moles) of docosapentaenoic acid in methylene chloride (10 mL) was treated with thionyl chloride (0.357 gm, 3×10−3 moles) and two drops of DMF. This solution was heated at 30° C. for two hours. After cooling the solvent and any unreacted thionyl chloride were removed under vacuum. The residue was added dropwise to a solution of budesonide (1.0 gm, 2.3×10−3 moles) in pyridine (10 mL) with stirring and ice cooling. After the addition was complete the reaction mixture was stirred at room temperature for one hour. Water (50 mL) containing 85% phosphoric acid (5 mL) was added and the insoluble material was extracted into diethyl ether (50 mL). After discarding the aqueous phase, the ether solution was washed with water (50 mL) containing 85% phosphoric acid (5 mL). The ether solution was dried over magnesium sulfate, then filtered and stripped under vacuum. The residue was purified by chromatograp...
example 3
Synthesis of the Eicosapentaenoic Acid Ester of Budesonide
[0022]A solution of 0.90 gm (3×10−3 moles) of eicosapentaenoic acid in methylene chloride (10 mL) was treated with thionyl chloride (0.357 gm, 3×10−3 moles) and two drops of DMF. This solution was heated at 30° C. for two hours. After cooling the solvent and any unreacted thionyl chloride were removed under vacuum. The residue was added dropwise to a solution of budesonide (1.0 gm, 2.3×10−3 moles) in pyridine (10 mL) with stirring and ice cooling. After the addition was complete the reaction mixture was stirred at room temperature for one hour. Water (50 mL) containing 85% phosphoric acid (5 mL) was added and the insoluble material was extracted into diethyl ether (50 mL). After discarding the aqueous phase, the ether solution was washed with water (50 mL) containing 85% phosphoric acid (5 mL). The ether solution was dried over magnesium sulfate, then filtered and stripped under vacuum. The residue was purified by chromatogra...
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