KR840007006A - Method for preparing pyrazolo [4,3-b] [1,4] oxazine - Google Patents

Abstract

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Description

Method for preparing pyrazolo [4,3-b] [1,4] oxazine

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Claims (10)

The compound of formula (II) is reacted with N, N-dialkylamide and phosphorus oxychloride of formula (VI) and the resulting salt is reacted with the general formula (IV) at a temperature of -20 ° C to 100 ° C. After reacting with hydrazine or acylating an oxazine of general formula (II) with a carboxylic acid ester of general formula (II), and sulfiding the resulting acyl product of general formula (VII), Method for preparing compounds of formula (Ia) and (Ib), characterized in that the reaction of the thion with the hydrazine of the general formula (IV) at a temperature of -20 to 100 ° C. In the above general formula R and R ¹ may be the same or different and are hydrogen, alkyl of 1 to 18 carbon atoms or phenyl [which may be alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, aralkyl of 7 to 22 carbon atoms, 6 to 6 carbon atoms; Aryl of 14, mono- and di-alkylamino of 1 to 12 carbon atoms, arylamino of 6 to 10 carbon atoms, aryloxy of 6 to 10 carbon atoms, alkylthio of 1 to 12 carbon atoms, arylthio of 6 to 10 carbon atoms 7-22 aralkyl, aralkylamino having 7 to 16 carbon atoms, carboxyl, caralkoxy having 2 to 13 carbon atoms, carbamoyl, mono- and di-alkylcarbamoyl having 1 to 12 carbon atoms, alkyl having 1 to 12 carbon atoms Sulfonyl, arylsulfonyl having 6 to 14 carbon atoms, halogenoalkyl having 12 or less carbon atoms, which is optionally mono- or multi-reduced by fluorine, chlorine, bromine and / iodine, hydroxy alkyl having 1 to 12 carbon atoms, C1-C12 aminoalkyl, C3 Alkoxycarbonylaminoalkyl having 13 moieties, halogenoalkoxy having up to 12 carbon atoms, which is optionally mono- or polysubstituted by fluorine, chlorine, bromine and / or iodine, halogen (e.g. fluorine, chlorine, bromine and iodine) , Amino, acylamino of 2 to 7 carbon atoms, carbamoyl amino, sulfonylamino, hydroxyl, acyloxy of 2 to 7 carbon atoms, sulfonamido, nitro, formyl, alkylcarbonyl of 2 to 13 carbon atoms, 7 carbon atoms Up to 5 identical or different substituents selected from the group consisting of arylcarbonyl, methylene carboxyl, methylene carboxyalkyl having 3 to 8 carbon atoms, ethylene carboxyalkyl having 4 to 9 carbon atoms, and propylene carboxyalkyl having 5 to 10 carbon atoms; Optionally substituted by R ² and R ³ may be the same or different, hydrogen; Or alkyl having 1 to 18 carbons which may be inserted with one or more oxygen, sulfur or nitrogen in the alkyl group; Alkenyl or alkynyl having 2 to 12 carbon atoms, arylalkyl having 7 to 12 carbon atoms (wherein alkenyl, alkynyl, and aralkyl groups may contain one or several oxygen, sulfur or nitrogen) or 6 to 14 carbon atoms 5- to 6-membered heteroaryl containing up to 4 lohete atoms selected from aryl, nitrogen, oxygen and sulfur of 1 to 12 carbon atoms in the alkyl side chain, and 4 selected from nitrogen, oxygen and sulfur 5- to 6-membered heteroarylalkyl containing up to 8 heteroatoms, alkylcarbonyl having 2 to 13 carbon atoms, arylcarbonyl having 7 to 15 carbon atoms, which is alkyl having 1 to 18 carbon atoms and having 3 to 6 cyclo atoms Alkyl, aralkyl of 7 to 22 carbon atoms, aryl of 9 to 14 carbon atoms, mono- and di-alkylamino carbon atoms of 1 to 12 carbon atoms, arylamino of 6 to 10 carbon atoms, aryloxy of 6 to 10 carbon atoms, and 1 to 12 carbon atoms. Alkylthio, carbon number Arylthio of 6 to 10, aralkyl of 7 to 22 carbon atoms, aralkyl amino of 7 to 16 carbon atoms, carboxyl, carboalkoxy of 2 to 13 carbon atoms, carbamoyl, mono- and di-alkyl carbamoyl of 1 to 12 carbon atoms , Alkylsulfonyl having 1 to 12 carbon atoms, arylsulfonyl having 6 to 14 carbon atoms, halogenoalkyl having 12 or less carbon atoms, which is optionally mono- or multi-substituted by fluorine, chlorine, and / or bromine or iodine Hydroxyalkyl having 1 to 12, aminoalkyl having 1 to 12 carbon atoms, alkoxycarbonyl aminoalkyl having 3 to 13 carbon atoms, and halogenoalkoxy having 12 or less carbon atoms, which is optionally mono- by fluorine, chlorine, bromine or / and iodine Or poly-substituted), halogen (eg fluorine, chlorine, bromine or / and iodine), amino, acylamino of 2 to 7 carbon atoms, sulfone amido, nitro, formyl, alkylcarbonyl of 2 to 18 carbon atoms, C7-C15 arylcarbonyl, methylene carboxy May optionally contain up to 5 identical or different substituents selected from methylenecarboxyalkyl having 3 to 8 carbon atoms, ethylene carboxyalkyl having 4 to 9 carbon atoms and propene carboxyalkyl having 4 or 9 selected from nitrogen, oxygen and sulfur; 5- to 6-heteroaryl aryl carbonyl containing up to 2 hetero atoms; R ⁵ is hydrogen, a straight chain, branched or cyclic alkyl group (each containing 1 to 6 carbon atoms, each of which is hydroxyl, carboxyl, formyl, acetyl, alkoxy, alkylthio, halogen, nitro, substituted amino group or May be optionally substituted by free amino group); An aromatic or heteroaromatic group containing up to 4 heteroatoms selected from nitrogen, oxygen, and sulfur and optionally optionally substituted by alkyl alkoxy, alkylthio or halogen; Similarly substituted aralkyl or heteroalkyl group, However, in general formula (IV) R ³ is hydrogen, alkyl of 1 to 18 carbon atoms, aralkyl of 7 to 12 carbon atoms, heteroalkyl, wherein one or several oxygen, sulfur and nitrogen may be inserted in the alkyl, aralkyl and hetero aralkyl group , Aryl or heteroaryl having 6 to 10 carbon atoms, wherein the aryl and heteroaryl groups are alkoxy, alkyl, aralkyl, cycloalkyl, aryl, alkylamino, dialkylamino, arylamino, aryloxy, arylthio, alkylthio, carboxyl 5 selected from carboalkoxy, cyano, carbamoyl, sulfonyl, alkylsulfonyl, halogenoalkyl, halogenoalkoxy, halogen, amino and substituted amino, sulfonamidomethylene, carboxyl, methylene carboxyalkyl and propylenecarboxyalkyl By the same or different tooth combinations below) ※ Note: It is to be disclosed based on the initial application.