KR890000499A - Method for preparing oxazinobenzothiazine 6,6-dioxide derivative - Google Patents

Abstract

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Description

Method for preparing oxazinobenzothiazine 6,6-dioxide derivative

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Claims (7)

5-Methyl-3-heteroaryl-2H, 5H-1,3-oxazino [5,6-c] [1,2] benzothiazine-2,4- (represented by the following general formula (I) In preparing 3H) -dione 6,6-dioxide, the amide represented by the following general formula (II) and the compound represented by the following general formula (III) are 4-methylaminopyridine and 4- (pyrrolidine-1 -Yl) oxazinobenzothiazine 6,6- characterized by reacting a substituted pyridine such as pyridine and 2,6-di-butyl-4-methylpyridine with an organic solvent selected from pyridine and mixtures thereof Method for producing a dioxide derivative. In the formulas (I), (II) and (III), R represents a heteroaryl group, preferably a substituted or unsubstituted pyrimidinyl or pyridyl group, R ¹ is a heteroarylamino group, preferably substituted or unsubstituted Ring pyrimidinylamino or pyridylamino group, R ² represents a C ₁ -C ₄ lower alkyl group such as methyl or ethyl, an aryl group such as phenyl or an alkylaryl group such as benzyl. The method of claim 1, wherein the reaction is carried out in a pyridine mixture containing 1 to 10% of at least one substituted pyridine. The method of claim 1, wherein the reaction is performed at a temperature of about −5 ° C. to 50 ° C. for about 3 to 48 hours. The amide according to any one of claims 1, 2 or 3, wherein R ¹ in general formula (II) is pyridin-2-ylamino and R ² in general formula (III) is an ethyl group. The compound was reacted in a pyridine solvent for 3 to 48 hours in the temperature range of -5 ° C to 40 ° C to give 5-methyl-3- (pyridin-2-yl) -2H, 5H-1,3-oxazino- [5 , 6-c] [1,2] Benzothiazine-2,4- (3H) -dione 6,6-dioxide. The amide according to any one of claims 1, 2 or 3, wherein R ¹ in general formula (II) is pyridin-2-ylamino and R ² in general formula (III) is a benzyl group. The compound was reacted in a pyridine solvent for 3 to 48 hours in the temperature range of -5 ° C to 40 ° C to give 5-methyl-3- (pyridin-2-yl) -2H, 5H-1,3-oxazino- [5 , 6-c] [1,2] Benzothiazine-2,4- (3H) -dione 6,6-dioxide. The amide according to any one of claims 1, 2 or 3, wherein R ¹ in general formula (II) is 4-methylpyridin-2-ylamino, and R ² in general formula (III). Is a phenyl group is reacted in 4-dimethylaminopyridine and pyridine solvent at a temperature of -5 ℃ to 40 ℃ for 3 to 48 hours to give 5-methyl-3- (pyridin-2-yl) -2H, 5H-1, 3-oxazino- [5,6-c] [1,2] benzothiazine-2,4- (3H) -dione 6,6-dioxide. The amide according to any one of claims 1, 2 or 3, wherein R ¹ in General Formula (II) is 6-methylpyridin-2-ylamino, and R ² in General Formula (III). Is a methyl group is reacted in 4-dimethylaminopyridine and pyridine solvent at a temperature of -5 ℃ to 40 ℃ for 3 to 48 hours to give 5-methyl-3- (pyridin-2-yl) -2H, 5H-1, 3-oxazino- [5,6-c] [1,2] benzothiazine-2,4- (3H) -dione 6,6-dioxide. ※ Note: The disclosure is based on the initial application.