5'----5--5'- NOVEL 5'-DEOXY-N-ALKYLOXYCARBONYL-5-FLUOROCYTOSINE-5'-THIOESTER DERIVATIVES THEIR PREPARATION AND ANTICANCER AGENT COMPRISING THE SAME

PURPOSE: 5'-Deoxy-N-alkyloxycarbonyl-5-fluorocytosine-5'-thioester derivatives, a preparation method thereof, an anticancer agent containing the same as effective components are provided. The compounds have improved anticancer effect and low toxicity. CONSTITUTION: 5'-deoxy-N-alkyloxy...

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Bibliographic Details
Main Authors KIM, GWAN HUI, LEE, GYEONG HO, KIM, YUN CHEOL, KIM, JI YEONG, PARK, HO JIN
Format Patent
LanguageEnglish
Korean
Published 31.01.2004
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:PURPOSE: 5'-Deoxy-N-alkyloxycarbonyl-5-fluorocytosine-5'-thioester derivatives, a preparation method thereof, an anticancer agent containing the same as effective components are provided. The compounds have improved anticancer effect and low toxicity. CONSTITUTION: 5'-deoxy-N-alkyloxycarbonyl-5-fluorocytosine-5'-thioester derivatives are represented by the formula(1), wherein R1 is hydrogen, or C1-C10 saturated or unsaturated carbohydrate; R2 is hydrogen, or atom group easily hydrolyzed under physiological condition or easily removable protecting group; and R3 is C2-C7 saturated or unsaturated carbohydrate. A method for preparing the 5'-deoxy-N -alkyloxycarbonyl-5-fluorocytosine-5'-thioester derivatives of the formula(1) comprises the steps of: (a) reacting a compound of the formula(2) with thiol of the formula(3) of R1-SH in the presence of a solvent to prepare a compound of the formula(1b); and (b) deprotecting the compound of the formula 1b. 본 발명은 신규 5'-데옥시-N-알킬옥시카르보닐-5-플루오로사이토신-5'-티오에스터 유도체 및 그의 제조방법에 관한 것으로, 보다 상세하게는 광범위한 5-FU 계열의 화합물과 그 유도체의 4'-위치에 메틸기 대신 티오에스터 유도체로 치환시켜 종래 항암제보다 우수한 항암활성을 가지는 5'-데옥시-N-알킬옥시카르보닐-5-플루오로사이토신-5'-티오에스터 유도체, 그의 제조방법, 및 이를 유효성분으로 포함하는 항암제에 관한 것이다.
Bibliography:Application Number: KR20020042046