Lipid-rich plaque regressing agents
a lipid-rich plaque and regressing agent technology, applied in the direction of biocide, drug composition, cardiovascular disorder, etc., can solve the problems of side effects, the inhibition of acat to reduce the intestinal absorption of cholesterol is not considered to be sufficient for regressing and removing the lipid-rich plaqu
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reference example 1
Synthesis of 6,7-dichloro-2-oxo-4-phenyl-2H-chromene-3-carboxylic acid
[0510]
A mixture of (4,5-dichloro-2-hydroxyphenyl) (phenyl)methanone (1.5 g), diethyl malonate (1.28 ml) and DBU (0.25 ml) was stirred at 170° C. for 30 minutes. The reaction mixture was dissolved in ethyl acetate (50 ml), and washed with water followed by a 1 N solution of hydrochloric acid and a saturated aqueous solution of sodium chloride. After drying over magnesium sulfate, the solvent was distilled off under reduced presurre, and the residue was purified by a column chromatography (packing: silica gel, eluent: ethyl acetate-hexane=1:9). The resultant crude product of ethyl 6,7-dichloro-2-oxo-4-phenyl-2H-chromene-3-carboxylate was dissolved in acetic acid (10 ml) and concentrated hydrochloric acid (5 ml), and heated under reflux for 1 hour. The reaction solution was concentrated under reduced pressure, and the resultant residue was dissolved in a solvent mixture of THF (10 ml) and ethyl acetate (50 ml), and...
reference example 2-6
[0516] The compounds of table 1 were obtained by the method similar to that in Reference Example 1.
TABLE 1Melting Point (° C.)Ref. Ex.Yield(RecrystallizationnumberR1R2R3(%)solvent)2ClMeH63227-228 (AcOEt)3ClMeMe58226-227 (AcOEt)4MeMeMe81205-206 (AcOEt)5MeMeMe27222-223 (AcOEt)6(CH2)4H 792-93 (AcOEt)
reference example 7
Synthesis of (6,7-dichloro-2-oxo-4-phenyl-2H-chromen-3-yl)acetic acid
[0517]
[0518] A solution of 6,7-dichloro-2-oxo-4-phenyl-2H-chromene-3-carboxylic acid (0.8 g) in THF (10 ml) was combined with DMF (1 drop) and oxalyl chloride (0.31 ml), and stirred at room temperature for 1 hour. After the reaction solution was concentrated under reduced pressure, the resultant residue was dissolved in THF (10 ml), and to which a solution of diazomethane prepared from N-methyl-N′-nitro-N-nitrosoguanidine (1.68 g) and potassium hydroxide (3.0 g) in ether (30 ml) was added dropwise. After the effervescence had ceased, the reaction solution was concentrated under reduced pressure. The resultant residue was dissolved in methanol (50 ml), combined with silver oxide, and heated under reflux for 30 minutes. After the insolubles were filtered off, the filtrate was concentrated under reduced pressure, and the residue was purified by a column chromatography (packing: silica gel, eluent: ethyl acetate-hexan...
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