Claims (2)
일반식General formula
(식중, R1은 할로겐원자ㆍ저급알킬기로 치환 또는 비치환된 페닐기를 나타내고, R2및 R3은 동일 또는 상이하여 수소원자, 할로겐원자, 저급알킬기를 나타낸다)로 나타내는 프로벤조이소옥사졸 유도체를 제조함에 있어,A probenzoisoxazole derivative represented by (wherein, R 1 represents a phenyl group unsubstituted or substituted with a halogen atom and a lower alkyl group, and R 2 and R 3 are the same or different and represent a hydrogen atom, a halogen atom or a lower alkyl group). In manufacturing,
a)일반식a) general formula
(식중, R1은 할로겐원자ㆍ저급알킬기로 치환 또는 비치환된 페닐기를 나타내고, R2및 R3은 동일 또는 상이하여 수소원자, 할로겐원자, 저급알킬기를 나타낸다)로 나타내는 벤조이소옥사졸 유도체에 포르말린 또는 그 유도체와 일반식(식중, R4및 R5는 저급알킬기를 나타낸다)을 반응시키든지 또는 포르말린 또는 그 유도체와 수산화알칼리를 반응시켜서 얻어지는 일반식:Formalin to a benzoisoxazole derivative represented by (wherein, R 1 represents a phenyl group unsubstituted or substituted with a halogen atom and a lower alkyl group, and R 2 and R 3 are the same or different and represent a hydrogen atom, a halogen atom, or a lower alkyl group). Or derivatives thereof and general formula (Wherein R 4 and R 5 represent a lower alkyl group) or by reacting formalin or a derivative thereof with alkali hydroxide:
(식중, R1은 할로겐원자ㆍ저급알킬기로 치환 또는 비치환된 페닐기를 나타내고, R2및 R3은 동일 또는 상이하여 수소원자, 할로겐원자, 저급알킬기를 나타내며, A는 -OH기 또는을 , R4및 R5는 저급알킬기를 나타낸다)로 나타내는 벤조이소옥사졸 유도체에 불활성 용매중 일반식 (R6)2S =CH-COOR7(식중, R6은 저급알킬기 또는 2-히드록시에틸기등의 치환 저금알킬기를, R7은 저급알킬기를 나타낸며, n은 0 또는 1의 정수이다)로 나타내는 화합물을 반응시키고 이어서 소망에 따라서 가수분해함을 특징으로 하는 제법.(Wherein R 1 represents a phenyl group unsubstituted or substituted with a halogen atom and a lower alkyl group, R 2 and R 3 are the same or different and represent a hydrogen atom, a halogen atom, a lower alkyl group, and A represents an —OH group or To a benzoisoxazole derivative represented by R 4 and R 5 as a lower alkyl group in a general formula (R 6 ) 2 S = CH-COOR 7 (wherein R 6 is a lower alkyl group or 2-hydroxyethyl group) in an inert solvent. And a substituted low alkyl group, such as R 7 represents a lower alkyl group, n is an integer of 0 or 1), and then hydrolyzes as desired.
b) 일반식b) general formula
(식중, R1은 할로겐원자ㆍ저급알킬기로 치환 또는 비치환된 페닐기를 나타내고, R2및 R3은 동일 또는 상이하여 수소원자, 할로겐원자, 저급알킬기를 나타낸다)로 나타내는 벤조이소옥사졸 유도체에 염기의 존재하 X-CH2-CH=CH2(식중 X은 할로겐원자를 나타낸다)을 반응시켜 일반식:Base in benjoyi sook Sasol derivative represented by: (wherein, R 1 represents a substituted or unsubstituted phenyl group with a halogen atom and a lower alkyl group, R 2 and R 3 represents a hydrogen atom, a halogen atom, a lower alkyl group, the same or different) X-CH 2 -CH = CH 2 (where X represents a halogen atom) in the presence of
(식중, R1,R2및 R3은 전기와 같은 것을 나타낸다)로 나타내는 화합물을 얻고 이를 용매하 가영에 의하여 전이시켜 일반식:(Wherein R 1 , R 2 and R 3 represent the same as the above), and the compound is converted by vaccination under solvent to give a general formula:
(식중, R1,R2및 R3은 전기와 같은 것을 나타낸다)로 나타내는 0-아릴 유도체를 생성하고, 이에 할로게노히드린화제를 반응시키고 이어서 염기로 처리하여 일반식:To yield a 0-aryl derivative represented by Formula 1 wherein R 1 , R 2 and R 3 represent the same as the above, and reacting the halogenohydrinizing agent followed by treatment with a base.
(식중, R1,R2및 R3은 전기와 같은 것을 나타낸다)로 나타내는 화합물을 제조하고, 이를 촉매하 과망간산 산화합을 특징으로 하는 제조방법.A process for producing a compound represented by the formula (wherein R 1 , R 2 and R 3 represent the same as the foregoing), and characterized in that the permanganic acid oxidation under the catalyst is carried out.
c) 일반식c) general formula
(식중, R1은 할로겐원자ㆍ저급알킬기로 치환 또는 비치환된 페닐기를 나타내고, R2및 R3은 동일 또는 상이하여 수소원자, 할로겐원자, 저급알킬기를 나타낸다)로 나타내는 벤조이소옥사졸 유도체에 일반식:General formula for the benzoisoxazole derivative represented by (wherein, R 1 represents a phenyl group unsubstituted or substituted with a halogen atom and a lower alkyl group, and R 2 and R 3 are the same or different and represent a hydrogen atom, a halogen atom or a lower alkyl group). expression:
CH2=CHC(OR4)3 CH 2 = CHC (OR 4 ) 3
(식중, R4는 저급알킬기를 나타낸다)로 나타내는 화합물을 반응시켜 일반식:(Wherein R 4 represents a lower alkyl group) by reacting a compound represented by the general formula:
(식중, R1,R2및 R3은 전기와 같은 것을 나타낸다)로 나타내는 화합물을 제조하고, 이어서 할로겐화제를 작용시키고 다시 가수분해함을 특징으로 하는 제법.A process characterized by preparing a compound represented by the formula (wherein R 1 , R 2 and R 3 represent the same as the former), and then reacting and hydrolyzing the halogenating agent.
d) 일반식d) general formula
(식중, R1은 할로겐원자ㆍ저급알킬기로 치환 또는 비치환된 페닐기를 나타내며, R2및 R3은 동일 또는 상이하여 수소원자, 할로겐원자, 저급알킬기를 나타내며, A는 -OH기 또는을 , R4는 저급아킬기를 나타낸다)로 나타내는 벤조이소옥사졸 유도체에 불활성 용매중 일반식 (R6)2S =CH-COOR7(식중, R6은 저급알킬기 또는 2-히드록시에틸기등의 치환 저금알킬기를, R7은 저급알킬기를 나타낸며, n은 0 또는 1의 정수이다)로 나타내는 화합물을 반응시키고, 이어서 소망에 따라서 가수분해함을 특징으로 하는 제법.(Wherein R 1 represents a phenyl group unsubstituted or substituted with a halogen atom and a lower alkyl group, R 2 and R 3 are the same or different and represent a hydrogen atom, a halogen atom, a lower alkyl group, and A represents an —OH group or Is substituted with a benzoisoxazole derivative represented by R 4 represents a lower alkyl group, in general formula (R 6 ) 2 S = CH-COOR 7 (wherein R 6 represents a lower alkyl group or 2-hydroxyethyl group, etc.) in an inert solvent. A lower alkyl group, R 7 represents a lower alkyl group, n is an integer of 0 or 1), followed by reacting the compound according to a desired process.
e) 일반식e) general formula
(식중, R1,R2및 R3은 전기와 같은 것을 나타낸다)로 나타내는 0-아릴페놀 유도체에 할로게노히드린화제를 반응시키고, 이어서 염기로 처리하여 일반식:The halogenohydrinizing agent is reacted with a 0-arylphenol derivative represented by formula (wherein R 1 , R 2 and R 3 represent the same as the above), followed by treatment with a base.
(식중, R1,R2및 R3은 전기와 같은 것을 나타낸다)로 나타내는 화합물을 제조하고, 이를 촉매하 과망간산 산화합을 특징으로 하는 제조방법.A process for producing a compound represented by the formula (wherein R 1 , R 2 and R 3 represent the same as the foregoing), and characterized in that the permanganic acid oxidation under the catalyst is carried out.
일반식General formula
(식중, R1은 할로겐원자ㆍ저급알킬기로 치환 또는 비치환된 페닐기를 나타내며, R2및 R3은 동일 또는 상이하여 수소원자, 할로겐원자, 저급알킬기를 나타내고, A는 -OH기 또는을, R4, 및 R5는 저급알킬기를 나타낸다)로 나타내는 벤조이소옥사졸 유도체.(Wherein R 1 represents a phenyl group unsubstituted or substituted with a halogen atom and a lower alkyl group, R 2 and R 3 are the same or different and represent a hydrogen atom, a halogen atom, a lower alkyl group, and A represents an —OH group or Benzoisoxazole derivatives represented by R < 4 > and R < 5 >
※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.