KR830005209A - Method for preparing benzoxazole and benzothiazole - Google Patents

Abstract

No content

Description

Method for preparing benzoxazole and benzothiazole

As this is a public information case, the full text was not included.

Claims (1)

a) closing the compound of formula (II) In the above structural formula R ₁ , R ₄ , R ₅ and X are as follows, Y represents a hydrogen atom or an acyl group, Z represents a nucleophilic substitutable group, b) reacting the carboxylic acid compounds of formula (III), their anhydrides, esters, thioesters, amides, imidazoles or halides with hydrazine Wherein R ₁ , R ₄ , R ₅ and X are as follows: c) A process for preparing benzoxazoles and benzthiazoles of the following formula (I) and their physiologically toxic salts, characterized by alkylating a compound of formula (IV) with a compound of formula (V). In the above structural formula R ₁ is a hydroxy or mercapto group optionally substituted by an alkyl group having 1 to 6 carbon atoms or an alkenyl group having 3 to 6 carbon atoms; The carbon atoms of the al moiety are 1 to 3 carbon atoms, and the phenyl nucleus may be mono-, di- or trisubstituted by an alkoxy group, a halogen atom and / or an amino group having 1 to 3 carbon atoms, and the substituents are the same or different from each other. Hydroxy or mercapto group substituted with; An alkyl group having 1 to 3 carbon atoms optionally substituted by a phenyl group; Phenyl group substituted with methoxy, cyano group or halogen atom; Or a group of the following structural formulas, here R ₂ is a hydrogen atom; Linear or branched chain groups having 1 to 7 carbon atoms which may be substituted with alkoxy groups having 1 to 3 carbon atoms; Cycloalkyl groups having 3 to 7 carbon atoms; Cycloalkyl groups which may be substituted by 1 or 2 alkoxy groups having 1 to 3 carbon atoms; Which may be substituted by alkyl or alkoxy groups having 1 to 3 carbon atoms, trifluoromethyl, nitro or cyano groups, fluorine, chlorine or bromine atoms and once again matched with these substituents, again having one or two carbon atoms An alkyl group of 3, an alkoxy group of 1 to 3 carbon atoms, or a phenyl group which may be substituted by fluorine, chlorine or bromine atom or the like; Or an alkoxycarbonyl group having 2 to 4 carbon atoms, R ₃ represents hydrogen or an alkyl group having 1 to 3 carbon atoms, R ₄ and R ₅ are the same or different groups and each represent an alkyl group having 1 to 3 carbon atoms, X represents oxygen or sulfur atom, A is hydroxy, mercapto or structural formula Represents a group of, Where R ₂ ′ represents the same as in R ₂ and R ₃ except for phenyl, R ₁ ′ is an alkyl group having 1 to 3 carbon atoms optionally substituted with phenyl or an alkoxy group having 1 to 3 carbon atoms, wherein the phenyl nucleus is an alkyl or alkoxy group having 1 to 3 carbon atoms, a halogen atom and / or an amino group as mono-, Can be di- or trisubstituted; Alkyl groups of 4 to 7 carbon atoms optionally substituted by alkoxy groups of 1 to 3 carbon atoms; Alkenyl groups having 3 to 6 carbon atoms; Or a cycloalkyl group having 3 to 7 carbon atoms, u represents a nucleophilic exchangeable group such as a halogen atom or sulfonic acid ester group, for example a chlorine, bromine or iodine atom, methanesulfonyloxy, p-toluene sulfonyloxy or methoxysulfonyloxy group. ※ Note: The disclosure is based on the initial application.