KR960014116A - New 1,4-dioxane derivatives and preparation method thereof - Google Patents

New 1,4-dioxane derivatives and preparation method thereof Download PDF

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Publication number
KR960014116A
KR960014116A KR1019940027067A KR19940027067A KR960014116A KR 960014116 A KR960014116 A KR 960014116A KR 1019940027067 A KR1019940027067 A KR 1019940027067A KR 19940027067 A KR19940027067 A KR 19940027067A KR 960014116 A KR960014116 A KR 960014116A
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KR
South Korea
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
dioxan
hydroxymethyl
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KR1019940027067A
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Korean (ko)
Inventor
민경복
김정우
이종률
안순길
Original Assignee
김충환
주식회사 종근당
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Application filed by 김충환, 주식회사 종근당 filed Critical 김충환
Priority to KR1019940027067A priority Critical patent/KR960014116A/en
Priority to BR9510327A priority patent/BR9510327A/en
Priority to PCT/KR1995/000135 priority patent/WO1996012716A1/en
Priority to AU37103/95A priority patent/AU3710395A/en
Priority to EP95934881A priority patent/EP0869953A1/en
Priority to JP8513791A priority patent/JP3047045B2/en
Priority to US08/817,611 priority patent/US6034087A/en
Priority to CA002203262A priority patent/CA2203262A1/en
Publication of KR960014116A publication Critical patent/KR960014116A/en
Priority to MXPA/A/1997/002886A priority patent/MXPA97002886A/en

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Abstract

본 발명에 따르면, 하기식(I)로 표시되는 1,4-디옥산 환상 화합물이 제공된다.According to this invention, the 1, 4- dioxane cyclic compound represented by following formula (I) is provided.

(식중, R1,은 수소, 포스페이트 또는 포스포테이트이고, R2는 피리미딘 또는 퓨린 염기이다.)Wherein R 1 , is hydrogen, phosphate or phosphate, and R 2 is pyrimidine or purine base.

상기 화합물(I)은 하기식(II)의 화합물을 염기와 반응시킴으로써 수득될 수 있으며, 화합물(I)의 합성 중간체인 식(II)의 화합물도 신규의 화합물로서 본 발명의 범위에 포함된다.The compound (I) can be obtained by reacting a compound of formula (II) with a base, and the compound of formula (II), which is a synthetic intermediate of compound (I), is also included in the scope of the present invention as a novel compound.

(식중, R7은 수소 또는 하이드록실기 보호기이고, L은 방향족 또는 비방향족 아실기, 할라이드기 또는 알콕시기이다.)(Wherein R 7 is a hydrogen or hydroxyl group protecting group, and L is an aromatic or non-aromatic acyl group, halide group or alkoxy group.)

Description

새로운 1,4-디옥산 유도체 및 그 제조방법New 1,4-dioxane derivatives and preparation method thereof

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

Claims (13)

하기 일반식(I)의 1,4-디옥산 화합물 유도체 및 약제학적으로 허용되는 그의 염.1,4-dioxane compound derivative of the following general formula (I), and a pharmaceutically acceptable salt thereof. 식중, R1,은 수소, 포스페이트 또는 포스포테이트이고, R2는 피리미딘 또는 퓨린 염기이다.Wherein R 1 , is hydrogen, phosphate or phosphate and R 2 is pyrimidine or purine base. 제1항에 있어서, 상기 일반식(I)의 화합물의 시스 이성체 및 약제학적으로 허용되는 그의 염.The cis isomer of the compound of formula (I) and a pharmaceutically acceptable salt thereof. 제1항에 있어서, 상기 일반식(I)의 화합물의 하나의 대장체 및 약제학적으로 허용되는 그의 염.The coli of the compound of formula (I) and a pharmaceutically acceptable salt thereof according to claim 1. 제1항에 있어서, 상기 일반식(I)의 R2가 우라실-1일, 시아민-1-일, 5-플루오로우라실-1일, 5-브로모우살실-1-일, 5-요오도우라실-1-일, 사이토신-1-일, 5-메틸사이토신-1-일, 5-풀루오로사이토신-1-일, 6-하이드록시퓨린-9-일, 퓨린-9-일, 2,6-디아미노퓨린-9-일, 2-아미노-6-클로로퓨린-9-일, 또는 구아닌-9-일인 화합물의 및 약제학적으로 허용되는 그의 염.A compound according to claim 1, wherein R 2 in formula (I) is uracil-l-yl, cyamine-l-yl, 5-fluorouracil-l-yl, 5-bromosalsil-l-yl, 5-io Douracil-1-yl, cytosine-1-yl, 5-methylcytosine-1-yl, 5- pullurocytosine-1-yl, 6-hydroxypurin-9-yl, purine-9- And pharmaceutically acceptable salts thereof of the compound which is 1, 2,6-diaminopurin-9-yl, 2-amino-6-chloropurin-9-yl, or guanine-9-yl. 제1항에 있어서, 1-(5-하이드록시메틸-1,4-디옥산-2-일)사이토신인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof of claim 1, which is 1- (5-hydroxymethyl-1,4-dioxan-2-yl) cytosine. 제1항에 있어서, 1-(5-하이드록시메틸-1,4-디옥산-2-일)시아민인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof according to claim 1, which is 1- (5-hydroxymethyl-1,4-dioxan-2-yl) cyamine. 제1항에 있어서, 1-(5-하이드록시메틸-1,4-디옥산-2-일)-5-클로로우라실인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof according to claim 1, which is 1- (5-hydroxymethyl-1,4-dioxan-2-yl) -5-chlorouracil. 제1항에 있어서, 1-(5-하이드록시메틸-1,4-디옥산-2-일)-5플루오로우라실인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof of claim 1, which is 1- (5-hydroxymethyl-1,4-dioxan-2-yl) -5fluorouracil. 제1항에 있어서, 2-아미노-6-클로로-9-(5-하이드록시메틸-1,4-디옥산-2-일)퓨린인 화합물 및 약제학적으로 허용되는 그의 염.The compound according to claim 1, which is 2-amino-6-chloro-9- (5-hydroxymethyl-1,4-dioxan-2-yl) purine, and a pharmaceutically acceptable salt thereof. 제1항에 있어서, 9-(5-하이드록시메틸-1,4-디옥산-2-일)구아닌인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof according to claim 1, which is 9- (5-hydroxymethyl-1,4-dioxan-2-yl) guanine. 제1항에 있어서, 9-(5-하이드록시메틸-1,4-디옥산-2-일)아데닌인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof according to claim 1, which is 9- (5-hydroxymethyl-1,4-dioxan-2-yl) adenine. 하기 일반식(II)의 1,4-디옥산 화합물.1,4-dioxane compound of the following general formula (II). 식중, R1,은 수소, 또는 하이드록실기 보호기이고, L은 방향족 또는 비방향족 아실기, 할라이드기 또는 알콕시기이다.Wherein R 1 , is hydrogen or a hydroxyl group protecting group, and L is an aromatic or non-aromatic acyl group, halide group or alkoxy group. 하기 일반식(II)의 화합물 염기 R2H와 반응시켜 하기 일반식(I)의 화합물을 제조하는 방법.A method for preparing a compound of formula (I) by reacting with a compound base R 2 H of formula (II). 식중, R1,은 수소, 포스페이트 또는 포스포테이트이고, R2는 피리미딘 또는 퓨린 염기이며, 식중, R7,은 수소, 또는 하이드록실기 보호기이고, L은 방향족 또는 비방향족 아실기, 할라이드기 또는 알콕시기이다.Wherein R 1 , is hydrogen, phosphate or phosphate, R 2 is a pyrimidine or purine base, wherein R 7 , is hydrogen, or a hydroxyl group protecting group, L is an aromatic or non-aromatic acyl group, halide Group or an alkoxy group. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019940027067A 1994-10-22 1994-10-22 New 1,4-dioxane derivatives and preparation method thereof KR960014116A (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
KR1019940027067A KR960014116A (en) 1994-10-22 1994-10-22 New 1,4-dioxane derivatives and preparation method thereof
BR9510327A BR9510327A (en) 1994-10-22 1995-10-21 Nucleoside derivatives and their preparation process
PCT/KR1995/000135 WO1996012716A1 (en) 1994-10-22 1995-10-21 Nucleoside derivatives and process for preparing thereof
AU37103/95A AU3710395A (en) 1994-10-22 1995-10-21 Nucleoside derivatives and process for preparing thereof
EP95934881A EP0869953A1 (en) 1994-10-22 1995-10-21 Nucleoside derivatives and process for preparing thereof
JP8513791A JP3047045B2 (en) 1994-10-22 1995-10-21 Nucleoside derivative and method for producing the same
US08/817,611 US6034087A (en) 1994-10-22 1995-10-21 Nucleoside derivatives and process for preparing thereof
CA002203262A CA2203262A1 (en) 1994-10-22 1995-10-21 Nucleoside derivatives and process for preparing thereof
MXPA/A/1997/002886A MXPA97002886A (en) 1994-10-22 1997-04-21 Nucleosid derivatives and process for preparation

Applications Claiming Priority (1)

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KR1019940027067A KR960014116A (en) 1994-10-22 1994-10-22 New 1,4-dioxane derivatives and preparation method thereof

Publications (1)

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KR960014116A true KR960014116A (en) 1996-05-22

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