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1. 发明专利

JPS58216169A 5-fluorouracil derivative and its preparation 失效
标题翻译： 5-氟尿嘧啶衍生物及其制备
公开(公告)号：JPS58216169A
公开(公告)日：1983-12-15
申请号：JP10097182
申请日：1982-06-11
申请人： Tanabe Seiyaku Co Ltd
发明人： INOUE KAZUMI , IWASAKI TAMEO , NISHITANI TAKASHI , KONDOU KAZUHIKO , ARAI YOSHIHISA
IPC分类号： C07D239/553 , A61K31/505 , A61P35/00 , C07D239/54
摘要： NEW MATERIAL:5-Fluorouracil derivative of formula I (R
1 is H, 1W15C alkyl, lower alkyl substituted with lower alkoxy; R
2 is formyl, lower alkanoyl, halogen-substituted lower alkanoyl; R
3 is lower alkyl, lower alkyl substituted with phenyl-lower-alkoxy; R
4 is lower alkyl, lower alkyl substituted with phenyl- lower-alkoxy) or its salt.
EXAMPLE: N-Acetyl-N-methyl-2-(5-fluorouracil-1-yl)glycine ethyl ester.
USE: Since it has antitumor activity, it is used as a medicine.
PREPARATION: The reaction between 2,4-bis(trimethylsilyl)-5-fluorouracil and a compound of formula II (R
5 is H, 1W5C alkyl; R
6 is formyl; R
7 is lower alkyl; R
8 is lower alkyl; Z is lower alkanoyloxy) in the presence of a Lewis acid gives the compound of formula I .
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式I的5-氟尿嘧啶衍生物（R 1是H，1-15C烷基，被低级烷氧基取代的低级烷基; R 2是甲酰基，低级烷酰基，卤素取代的低级烷酰基; R 3，是低级烷基，被苯基 - 低级烷氧基取代的低级烷基; R 4是低级烷基，被苯基 - 低级烷氧基取代的低级烷基）或其盐。实施例：N-乙酰基-N-甲基-2-（5-氟尿嘧啶-1-基）甘氨酸乙酯。用途：由于具有抗肿瘤活性，用作药物。制备：2,4-双（三甲基甲硅烷基）-5-氟尿嘧啶与式II化合物（R 5）之间的反应是H，1-5C烷基; R 6是甲酰基; R 7是低级烷基 ; R 8为低级烷基; Z为低级烷酰氧基），在路易斯酸存在下，得到式I化合物。

2. 发明专利

JPS5927876A 5-fluorouracil derivative and its preparation 失效
标题翻译： 5-氟尿嘧啶衍生物及其制备
公开(公告)号：JPS5927876A
公开(公告)日：1984-02-14
申请号：JP13708882
申请日：1982-08-05
申请人： Tanabe Seiyaku Co Ltd
发明人： MIYOSHI SOUJI , INOUE KAZUMI , MUSHISHIKA YOSHITAKA , IWASAKI TAMEO , NISHITANI TAKASHI , ARAI YOSHIHISA
IPC分类号： C07D239/553 , A61K31/505 , A61P35/00
摘要： NEW MATERIAL:A compound shown by the formula I (R
1 is lower alkyl, or lower alkenyl; R
2 is lower alkenyl, substituted lower alkyl, substituted-aralkyl, etc.; R
3 is H, or lower alkoxycarbonyl) and its pharmaceutically acceptable salts.
EXAMPLE: N-Methoxyacetyl-2-(5-fluorouracil-1-yl)leucine ethyl ester.
USE: An antitumor agent.
PROCESS: A compound shown by the formula III (R
4 is lower alkenyl, substituted lower alkyl, substituted-aralkyl, etc.; Y is lower alkoxy, or lower alkanoyloxy) is reacted with a compound shown by the formula II in the presence of Lewis acid, or a compound shown by the formula III (Z is lower alkanoyloxy) is reacted with a compound shown by the formula IV in the presence of an alkali metal hybride, to give the desired compound.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：由式I表示的化合物（R 1是低级烷基或低级烯基; R 2是低级链烯基，取代的低级烷基，取代的 - 芳烷基等; R 3是H或低级烷氧基羰基）及其药学上可接受的盐。实施例：N-甲氧基乙酰基-2-（5-氟尿嘧啶-1-基）亮氨酸乙酯。用途：抗肿瘤剂。方法：式Ⅲ化合物（R 4为低级链烯基，取代的低级烷基，取代的芳烷基等; Y为低级烷氧基或低级烷酰氧基）与式II所示的化合物反应在碱金属混合物存在下，将路易斯酸或式III化合物（Z为低级烷酰氧基）的存在与式Ⅳ所示的化合物反应得到所需化合物。

3. 发明专利

JPS58213762A 5-fluorouracil derivative and preparation thereof 失效
标题翻译： 5-氟尿嘧啶衍生物及其制备方法
公开(公告)号：JPS58213762A
公开(公告)日：1983-12-12
申请号：JP9670982
申请日：1982-06-04
申请人： Tanabe Seiyaku Co Ltd
发明人： MIYOSHI SOUJI , INOUE KAZUMI , MUSHISHIKA YOSHITAKA , IWASAKI TAMEO , NISHITANI TAKASHI , ARAI YOSHIHISA
IPC分类号： C07D239/553 , A61K31/505 , A61P35/00 , C07D239/54 , C07D403/06 , C07D405/06
摘要： NEW MATERIAL:A compound expressed by formula I (R
1 is lower alkoxyl, lower alkoxy-substituted lower alkoxyl, lower cycloalkyl, lower cycloalkyloxy, lower alkoxycarbonyl or benzyloxycarbonyl, etc.; R
2 is H or lower alkyl; R
3 is lower alkyl; A is lower alkylene) or a salt thereof.
EXAMPLE: N-Acetyl-2-isopropoxymethyl-2-(5-fluorouracil-1-yl)glycine ethyl ester.
USE: A medicine having antitumor action.
PROCESS: A compound expressed by formula II (R
4 is lower alkoxyl, lower alkoxy-substituted lower alkoxyl, lower cycloalkyl, etc.; R
5 is lower alkanoyl) is reacted with a 2,4-bistrimethylsilyl-5-fluorouracil expressed by formula III in a solvent in the presence of a Lewis acid to afford the compound expressed by formula I (R
1 is R
4 ).
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：由式I表示的化合物（R 1）为低级烷氧基，低级烷氧基取代的低级烷氧基，低级环烷基，低级环烷氧基，低级烷氧基羰基或苄氧羰基等; R 2为H或低级烷基; R 3为低级烷基; A为低级亚烷基）或其盐。实施例：N-乙酰基-2-异丙氧基甲基-2-（5-氟尿嘧啶-1-基）甘氨酸乙酯。用途：具有抗肿瘤作用的药物。方法：由式II表示的化合物（R 4是低级烷氧基，低级烷氧基取代的低级烷氧基，低级环烷基等; R 5是低级烷酰基）与2,4-双三甲基甲硅烷基-5- 在路易斯酸存在下，在溶剂中由式III表示的氟尿嘧啶，得到由式I表示的化合物（R 1为R 4）。

4. 发明专利

JPS58222071A 5-fluorouracil derivative and its preparation 失效
标题翻译： 5-氟尿嘧啶衍生物及其制备
公开(公告)号：JPS58222071A
公开(公告)日：1983-12-23
申请号：JP10514382
申请日：1982-06-17
申请人： Tanabe Seiyaku Co Ltd
发明人： MIYOSHI SOUJI , INOUE KAZUMI , MUSHISHIKA YOSHITAKA , IWASAKI TAMEO , NISHITANI TAKASHI , ARAI YOSHIHISA
IPC分类号： C07D239/553 , A61K31/505 , A61P35/00 , C07D239/54
摘要： NEW MATERIAL:The 5-fluorouracil derivative of formula I [R
1 and R
2 are lower alkyl; R
3 is OR
4 (R
4 is alkenyl, alkynyl, etc.) or NR
5 R
6 (R
5 is H or alkyl; R
6 is alkyl, monoalkoxycarbonyl-substituted alkyl, etc.)] or its pharmacologically permissible salt.
EXAMPLE: N-Acetyl-2-(5-fluorouracil-1-yl)leucine 2-methoxyethyl ester.
USE: Antitumor agent.
PROCESS: The compound of formula I -a which is one of the compound of formula I , can be prepared, e.g. by reacting 2,4-bistrimethylsilyl-5-fluorouracil of formula II with the compound of formula III (R
7 is alkanoyl; R
8 is alkoxy- substituted alkyl) in the presence of a Lewis acid, and if desired, converting the product to a pharmacologically permissible salt.
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式Ⅰ的5-氟尿嘧啶衍生物[R 1和R 2]为低级烷基; R 3是OR 4（R 4是烯基，炔基等）或NR 5 R 6（R 5是H或烷基; R 6是烷基，单烷氧基羰基 - 取代的烷基等）]或其药理学上允许的盐。实施例：N-乙酰基-2-（5-氟尿嘧啶-1-基）亮氨酸2-甲氧基乙酯。用途：抗肿瘤剂。方法：可以制备作为式I化合物之一的式I-a化合物，例如通过在路易斯酸的存在下，使式II的2,4-双三甲基甲硅烷基-5-氟尿嘧啶与式III化合物（R 7是烷酰基; R 8是烷氧基取代的烷基）反应，如果需要，将产品转化为药理学上允许的盐。

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