KR960014117A - New 1,4-oxatian derivatives and preparation method thereof - Google Patents

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

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Publication number
KR960014117A
KR960014117A KR1019940027068A KR19940027068A KR960014117A KR 960014117 A KR960014117 A KR 960014117A KR 1019940027068 A KR1019940027068 A KR 1019940027068A KR 19940027068 A KR19940027068 A KR 19940027068A KR 960014117 A KR960014117 A KR 960014117A
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KR
South Korea
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
hydroxymethyl
formula
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Application number
KR1019940027068A
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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 KR1019940027068A priority Critical patent/KR960014117A/en
Priority to PCT/KR1995/000135 priority patent/WO1996012716A1/en
Priority to BR9510327A priority patent/BR9510327A/en
Priority to EP95934881A priority patent/EP0869953A1/en
Priority to JP8513791A priority patent/JP3047045B2/en
Priority to AU37103/95A priority patent/AU3710395A/en
Priority to CA002203262A priority patent/CA2203262A1/en
Priority to US08/817,611 priority patent/US6034087A/en
Publication of KR960014117A publication Critical patent/KR960014117A/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-옥사티안 유도체가 제공된다.According to this invention, the 1, 4-oxatian derivative represented by following formula (I) is provided.

(식중, R1,은 수소, 포스페이트 또는 포스포테이트이고, R2는 피리미딘 또는 퓨린 염기이며, Z는 S, SO, 또는 SO2이다.)Wherein R 1 , is hydrogen, phosphate or phosphate, R 2 is a pyrimidine or purine base, and Z is S, SO, or SO 2 .

상기 화합물(I)은 하기식(II)의 화합물을 염기화 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 basifying the compound of formula (II), 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, R7,은 수소, 또는 하이드록실기 보호기이고, L은 방향족 또는 비방향족 아실기, 할라이드기 또는 알콕시기이며, Z는 S, SO, 또는 SO2이다.)(Wherein R 7 is a hydrogen or hydroxyl group protecting group, L is an aromatic or non-aromatic acyl group, halide group or alkoxy group, and Z is S, SO, or SO 2. )

Description

새로운 1,4-옥사티안 유도체 및 그 제조방법New 1,4-oxatian 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-옥사티안 화합물 유도체 및 약제학적으로 허용되는 그의 염.1,4-oxatian 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 염기이며, Z는 S, SO, 또는 SO2이다.Wherein R 1 , is hydrogen, phosphate or phosphate, R 2 is a pyrimidine or purine base, and Z is S, SO, or SO 2 . 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-클로로우라실-1-일, 5-브로모우라실-1-일, 5-요요오드우라실-1-일, 사이토신-1-일, 5-메틸사이토신-1-일, 5-플루오르사이토신-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-1 yl, cyamine-1-yl, 5-fluorouracil-1 yl, 5-chlorouracil-1 yl, 5-bromo Uracil-1-yl, 5-iodouracil-1-yl, cytosine-1-yl, 5-methylcytosine-1-yl, 5-fluorocytosine-1-yl, 6-hydroxypurin-9 And pharmaceutically acceptable salts of compounds that are -yl, purin-9-yl, 2,6-diaminopurin-9-yl, 2-amino-6-chloropurin-9-yl, or guanine-9-yl . 제1항에 있어서, 1-(5-하이드록시메틸-1,4-옥사티안-2-일)사이토신인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof according to claim 1, which is 1- (5-hydroxymethyl-1,4-oxatian-2-yl) cytosine. 제1항에 있어서, 1-(5-하이드록시메틸-1,4-옥사티안-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-oxatian-2-yl) cyamine. 제1항에 있어서, 1-(5-하이드록시메틸-1,4-옥산티안-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-oxanthanti-2-yl) -5-chlorouracil. 제1항에 있어서, 1-(5-하이드록시메틸-1,4-옥산이찬-2-일)-5플루오로우라실인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof according to claim 1, which is 1- (5-hydroxymethyl-1,4-oxandi-2-yl) -5fluorouracil. 제1항에 있어서, 2-아미노-6-클로로-9-(5-하이드록시메틸-1,4-옥산티안-2-일)퓨린인 화합물 및 약제학적으로 허용되는 그의 염.The compound and pharmaceutically acceptable salt thereof according to claim 1, which is 2-amino-6-chloro-9- (5-hydroxymethyl-1,4-oxanthanti-2-yl) purine. 제1항에 있어서, 9-(5-하이드록시메틸-1,4-옥산티안-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-oxanthanti-2-yl) guanine. 제1항에 있어서, 9-(5-하이드록시메틸-1,4-옥산티안-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-oxanthanti-2-yl) adenine. 하기 일반식(II)의 1,4-옥산티안 화합물.1,4-oxanthane compound of the following general formula (II). 식중, R7,은 수소, 또는 하이드록실기 보호기이고, L은 방향족 또는 비방향족 아실기, 할라이드기 또는 알콕시기이고, Z는 S, SO, 또는 SO2이다.Wherein R 7 is a hydrogen or hydroxyl group protecting group, L is an aromatic or non-aromatic acyl group, halide group or alkoxy group, and Z is S, SO, or SO 2 . 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 퓨린염기이며, Z는 S, SO, 또는 SO2또는 R7,은 수소, 또는 하이드록실기 보호기이고, L은 방향족 또는 비방향족 아실기, 할라이드기 또는 알콕시기이며, Z는 S, SO, 또는 SO2이다.Wherein R 1 , is hydrogen, phosphate or phosphate, R 2 is a pyrimidine or purine base, Z is S, SO, or SO 2 or R 7 , is hydrogen, or a hydroxyl group protecting group, L is Aromatic or non-aromatic acyl group, halide group or alkoxy group, Z is S, SO, or SO 2 . ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019940027068A 1994-10-22 1994-10-22 New 1,4-oxatian derivatives and preparation method thereof KR960014117A (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
KR1019940027068A KR960014117A (en) 1994-10-22 1994-10-22 New 1,4-oxatian derivatives and preparation method thereof
PCT/KR1995/000135 WO1996012716A1 (en) 1994-10-22 1995-10-21 Nucleoside derivatives and process for preparing thereof
BR9510327A BR9510327A (en) 1994-10-22 1995-10-21 Nucleoside derivatives and their preparation process
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
AU37103/95A AU3710395A (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
US08/817,611 US6034087A (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)

Application Number Priority Date Filing Date Title
KR1019940027068A KR960014117A (en) 1994-10-22 1994-10-22 New 1,4-oxatian derivatives and preparation method thereof

Publications (1)

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KR960014117A true KR960014117A (en) 1996-05-22

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