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Application filed by 폴 아드리안 쟌 쟈안센, 쟈안센 파아마슈우티카 엔. 브이.filedCritical폴 아드리안 쟌 쟈안센
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Publication of KR900001682ApublicationCriticalpatent/KR900001682A/en
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Claims (2)
구조식(III)의 화합물을 구조식(II)의 2-아미노 벤조산 에스테르로 불활성용매중에서 승은하에 폐환반응시켜, 구조식(I)의 3-[2-[4-(4-플루오로벤조일)-1-피페리디닐]에틸]-2,4(1H,3H)퀴나졸린디온 및 그 산부가염을 제조하는 방법.The compound of formula (III) is ring-closed with a 2-amino benzoic acid ester of formula (II) in an inert solvent under sublimation to give 3- [2- [4- (4-fluorobenzoyl) -1- Piperidinyl] ethyl] -2,4 (1H, 3H) quinazolindione and its acid addition salt.위에서, L1은 수소이고, L2는 반응성이탈기이다. L1및 L2는 함께 직접결합을 형성하고, R은 C1-6알킬 또는 아릴이다.In the above, L 1 is hydrogen and L 2 is a reactive leaving group. L 1 and L 2 together form a direct bond and R is C 1-6 alkyl or aryl.구조식(IV)의 아민을 수직식 L2-CO-L2(V)의 화합물로 과량의 구조식(V)의 화합물과함께 또는 불활성용매중에서 임의로 승온하에 처리하고, 생성한 구조식 (III)의 중간화합물을 구조식(III)의 2-아미노벤조산 에스테르로 불활성용매중에서 승온하에 폐환반응시켜, 구조식(I)의 3-[2-[4-(4-플루오로벤조일)-1-피페리디닐]에틸]-2,4(1H,3H)퀴나졸린디온 및 그 산부가염을 제조하는 방법.The amine of formula (IV) was treated with a compound of formula L 2 -CO-L 2 (V) with an excess of the compound of formula (V) or optionally at elevated temperature in an inert solvent, resulting in the intermediate of formula (III) The compound was cyclized to a 2-aminobenzoic acid ester of formula (III) at elevated temperature in an inert solvent to yield 3- [2- [4- (4-fluorobenzoyl) -1-piperidinyl] ethyl of formula (I). ] -2,4 (1H, 3H) quinazolindione and its acid addition salt.위에서, L1은 수소이고, L2는 반응성이탈기거나, L1및 L2는 함께 직접결합믈 형성하고, R은 C1-6알킬 또는 아릴이다.In the above, L 1 is hydrogen, L 2 is a reactive leaving group, or L 1 and L 2 together form a direct bond, R is C 1-6 alkyl or aryl.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
1- / 3- (2-DIALKYLAMINOETHOXY) -2-THENYL / -3-PHENYL-1-PROPANONER FOR THE SYRAADDITIONSSALTER, FOERFARANDE FOER DERAS FRAMSTAELLNING OCH DESSA INNEHAOLLANDE PHARMACEUTICAL SAMMANSAETTNINGAR.