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1. 发明授权

US5776929A Benzodiazepine derivative 失效
标题翻译：苯二氮卓衍生物
公开(公告)号：US5776929A
公开(公告)日：1998-07-07
申请号：US663304
申请日：1996-06-25
申请人： Sanji Hagishita , Susumu Kamata , Kaoru Seno , Nobuhiro Haga , Yasunobu Ishihara
发明人： Sanji Hagishita , Susumu Kamata , Kaoru Seno , Nobuhiro Haga , Yasunobu Ishihara
IPC分类号： C07D243/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14 , A61K31/55
CPC分类号： C07D403/12 , C07D243/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/14
摘要： A benzodiazepine derivative of the formula (I): ##STR1## wherein R.sub.1 is a bond, --CH.sub.2 --, --CH.sub.2 O--, --SCH.sub.2 -- or a group of the formula: ##STR2## R.sub.2 is a lower alkyl, --COOR.sub.5, --CONH(CH.sub.2).sub.n COOR.sub.5, --CONHSO.sub.2 R.sub.5, --SO.sub.2 NHCOR.sub.5, or an optionally substituted heterocyclic group (R.sub.5 is a hydrogen atom, lower alkyl or benzyl and n is an integer of 1 to 5); R.sub.3 is a bond, --CO-- or --CONH--; and R.sub.4 is an optionally substituted heterocyclic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.
摘要翻译： PCT No.PCT / JP94 / 02132 Sec。 371日期1996年6月25日第 102（e）日期1996年6月25日PCT 1994年12月19日PCT PCT。公开号WO95 / 18110 日期：1995年7月6日一种式（I）的苯并二氮杂衍生物：其中R 1是一个键，-CH 2 - ， - CH 2 O-，-SCH 2 - 或下式的基团：低级烷基，-COOR 5，-CONH（CH 2）n COOR 5，-CONHSO 2 R 5，-SO 2 NHCOR 5或任选取代的杂环基（R 5为氢原子，低级烷基或苄基，n为1至5的整数）。 R3是键，-CO-或-CONH-; 并且R4是任选取代的杂环基，任选取代的低级烷基，任选取代的低级环烷基，任选取代的芳基或低级烷氧基羰基或其药学上可接受的盐，其对胃泌素受体和/或CCK-B受体具有高亲和力但不适用于CCK-A受体，并且可用于治疗与胃泌素受体和/或CCK-B受体相关的疾病，而不诱导与CCK-A受体相关的副作用。

2. 发明授权

US4861913A Bicyclic sulfonamide derivatives 失效
标题翻译：双环磺酰胺衍生物
公开(公告)号：US4861913A
公开(公告)日：1989-08-29
申请号：US927823
申请日：1986-11-05
申请人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Sanji Hagishita , Kaoru Seno , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
发明人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Sanji Hagishita , Kaoru Seno , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
IPC分类号： C07D493/08 , A61K31/00 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/557 , A61P7/02 , A61P9/08 , A61P11/08 , C07C20060101 , C07C67/00 , C07C301/00 , C07C311/00 , C07C311/02 , C07C311/07 , C07C311/10 , C07C311/13 , C07C311/15 , C07C311/20 , C07C311/37 , C07C313/00 , C07C323/52 , C07D209/52 , C07D209/56 , C07D213/34 , C07D213/71 , C07D221/22 , C07D303/40 , C07D303/46 , C07D331/02 , C07D491/044 , C07D493/04 , C07D495/04
CPC分类号： C07D493/08 , C07D213/34 , Y02P20/55
摘要： Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or heterocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms an may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.
摘要翻译：由下式表示的双环磺酰氨基衍生物：其中R1是氢或低级烷基; R2是烷基，取代或未取代的芳基，芳烷基或杂环基; R3是氢或甲基; X是可以被氟原子或原子取代的亚烷基或亚烯基，链中可以含有氧，硫和/或亚苯基; Y是直链或支链亚烷基或亚烯基，氧或硫; m为0或1; 并且n为0,1或2或其盐，所述衍生物可用作抗血栓形成，抗血管收缩和抗支气管收缩药物。

3. 发明授权

US5138067A Lipid derivatives 失效
标题翻译：脂质衍生物
公开(公告)号：US5138067A
公开(公告)日：1992-08-11
申请号：US707164
申请日：1991-05-29
申请人： Susumu Kamata , Tatsuo Tsuri , Nobuhiro Haga , Takeaki Matsui , Morio Kishi , Kimio Takahashi , Sanji Hagishita , Kaoru Seno
发明人： Susumu Kamata , Tatsuo Tsuri , Nobuhiro Haga , Takeaki Matsui , Morio Kishi , Kimio Takahashi , Sanji Hagishita , Kaoru Seno
IPC分类号： C07C311/32 , C07C311/46 , C07C323/49 , C07C391/00 , C07D213/20 , C07D215/10 , C07D217/10 , C07D241/12 , C07D261/12 , C07D277/22 , C07D277/62 , C07D295/088 , C07D413/12 , C07D521/00
CPC分类号： C07D213/20 , C07C311/32 , C07C311/46 , C07C323/49 , C07C391/00 , C07D215/10 , C07D217/10 , C07D231/12 , C07D233/56 , C07D241/12 , C07D249/08 , C07D261/12 , C07D277/22 , C07D277/62 , C07D295/088 , C07D413/10
摘要： Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or heterocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together with R.sub.2 form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.
摘要翻译：由下式表示的脂质衍生物：其中R1是烷基或烷基氨基甲酰基; 低级烷氧基羰基氨基，低级烷基脲基，低级烷氧基甲基，低级烷基羰基甲基，氰基甲基，杂环基或杂环氧基; R2'是氢或R2和R2'与R2一起形成-O（CH 2）m - ，其中m是1至5的整数; R 3，R 4和R 5各自为氢或低级烷基或R 3，R 4和R 5中的两个或三个与相邻的氮原子一起形成环状铵; R6是氢或低级烷基羰基; X-是抗衡阴离子; Y是氧或硫; n为1〜10的整数，可用作PAF拮抗剂，例如作为抗血栓形成，抗收缩性抗静电收缩剂或抗肿瘤剂。

4. 发明授权

US4960909A 7-oxabicyclo[2.2.1] heptane sulfonamide derivatives 失效
标题翻译： 7-氧杂二环[2.2.1]庚烷磺酰胺衍生物
公开(公告)号：US4960909A
公开(公告)日：1990-10-02
申请号：US327772
申请日：1989-03-23
申请人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Sanji Hagishita , Kaoru Seno , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
发明人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Sanji Hagishita , Kaoru Seno , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
IPC分类号： C07D493/08 , A61K31/00 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/557 , A61P7/02 , A61P9/08 , A61P11/08 , C07C20060101 , C07C67/00 , C07C301/00 , C07C311/00 , C07C311/02 , C07C311/07 , C07C311/10 , C07C311/13 , C07C311/15 , C07C311/20 , C07C311/37 , C07C313/00 , C07C323/52 , C07D209/52 , C07D209/56 , C07D213/34 , C07D213/71 , C07D221/22 , C07D303/40 , C07D303/46 , C07D331/02 , C07D491/044 , C07D493/04 , C07D495/04
CPC分类号： C07D493/08 , C07D213/34 , Y02P20/55
摘要： Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or hetelocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms and may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.

5. 发明授权

US5739162A Carbamoylmethylurea derivatives 失效
标题翻译：氨基甲酰基甲基脲衍生物
公开(公告)号：US5739162A
公开(公告)日：1998-04-14
申请号：US687433
申请日：1996-08-09
申请人： Sanji Hagishita , Susumu Kamata , Yasushi Murakami , Nobuhiro Haga , Yasunobu Ishihara , Toshiro Konoike
发明人： Sanji Hagishita , Susumu Kamata , Yasushi Murakami , Nobuhiro Haga , Yasunobu Ishihara , Toshiro Konoike
IPC分类号： A61K31/17 , A61K38/00 , A61K38/05 , A61P1/04 , C07C275/28 , C07K5/06 , C07K5/062 , A61K31/24
CPC分类号： C07K5/0606 , C07C275/28 , C07K5/06026 , C07K5/06139 , A61K38/00
摘要： A compound of the formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or lower alkyl; R.sub.2 is a lower alkoxy, lower alkylamino, lower cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclic group; R.sub.3 is an optionally substituted phenyl; R.sub.4 is an optionally substituted phenyl, optionally substituted cycloalkyl, optionally substituted alkyl or optionally substituted heterocyclic group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.
摘要翻译： PCT No.PCT / JP95 / 00161 Sec。 371日期：1996年8月9日 102（e）日期1996年8月9日PCT提交1995年2月7日PCT公布。 WO95 / 21856 PCT公开日期：1995年8月17日一种式（I）化合物：其中R 1是氢原子或低级烷基; R2是低级烷氧基，低级烷基氨基，低级环烷基，任意取代的苯基或任意取代的杂环基; R3是任选取代的苯基; R4是任选取代的苯基，任选取代的环烷基，任选取代的烷基或任选取代的杂环基，或其药学上可接受的盐，其对胃泌素受体和/或CCK-B受体具有高亲和力，但不对CCK-A受体具有高亲和力，并且可用于治疗与胃泌素受体和/或CCK-B受体相关的疾病，而不诱导与CCK-A受体相关的副作用。

6. 发明授权

US5047540A Lipid derivatives 失效
标题翻译：脂质衍生物
公开(公告)号：US5047540A
公开(公告)日：1991-09-10
申请号：US284590
申请日：1988-11-29
申请人： Susumu Kamata , Tatsuo Tsuri , Nobuhiro Haga , Takeaki Matsui , Morio Kishi , Kimio Takahashi , Sanji Hagashita , Kaoru Seno
发明人： Susumu Kamata , Tatsuo Tsuri , Nobuhiro Haga , Takeaki Matsui , Morio Kishi , Kimio Takahashi , Sanji Hagashita , Kaoru Seno
IPC分类号： C07C311/32 , C07C311/46 , C07C323/49 , C07C391/00 , C07D213/20 , C07D215/10 , C07D217/10 , C07D241/12 , C07D249/14 , C07D261/12 , C07D277/22 , C07D277/62 , C07D295/088 , C07D413/12 , C07D521/00
CPC分类号： C07D213/20 , C07C311/32 , C07C311/46 , C07C323/49 , C07C391/00 , C07D215/10 , C07D217/10 , C07D231/12 , C07D233/56 , C07D241/12 , C07D249/08 , C07D261/12 , C07D277/22 , C07D277/62 , C07D295/088 , C07D413/12
摘要： Lipid derivatives represented by the formula: ##STR1## wherein R.sub.1 is alkyl or alkylcarbamoyl; R.sub.2 is lower alkyloxy, lower alkylcarbamoyloxy, lower alkylcarbonylamino, lower alkyloxycarbonylamino, lower alkylureido, lower alkyloxymethyl, lower alkylcarbonylmethyl, cyanomethyl, heterocyclic group, or he0 terocyclyloxy; R.sub.2 ' is hydrogen or R.sub.2 and R.sub.2 ' taken together form --O(CH.sub.2).sub.m -- wherein m is an integer of 1 to 5; R.sub.3, R.sub.4, and R.sub.5 each is hydrogen or lower alkyl or two or three of R.sub.3, R.sub.4, and R.sub.5 taken together with the adjacent nitrogen atom form cyclic ammonio; R.sub.6 is hydrogen or lower alkylcarbonyl; X.sup.- is a counter anion; Y is oxygen or sulfur; and n is an integer of 1 to 10, being useful as PAF antagonists, e.g., as antithrombotic, antivasoconstricting, antibronchoconstricting agent or antitumor agent.

7. 发明授权

US5463052A Method for producing benzylidene derivatives 失效
标题翻译：亚苄基衍生物的制备方法
公开(公告)号：US5463052A
公开(公告)日：1995-10-31
申请号：US246494
申请日：1994-05-20
申请人： Nobuhiro Haga , Masanao Inagaki , Saichi Matsumoto , Susumu Kamata
发明人： Nobuhiro Haga , Masanao Inagaki , Saichi Matsumoto , Susumu Kamata
IPC分类号： C07D207/26 , C07D265/02 , C07D275/02 , C07D279/02 , C07D281/02 , C07D281/18 , C07D291/00 , C07D291/04 , C07D291/06
CPC分类号： C07D275/02 , C07D265/02 , C07D291/06 , Y02P20/55
摘要： A selective and high-yield method is described for producing stereoisomeric benzylidene derivatives of the formula III: ##STR1## wherein R.sup.1 and R.sup.2 each independently is lower alkyl, lower alkoxy or halogen; Y is SO.sub.2, SO or CO; --A-- is optionally substituted lower alkylene; --B-- is --CH.sub.2 -- or --O--; or --A-- and --B-- taken together may form optionally substituted phenylene or optionally substituted lower alkenylene; and R is hydrogen, optionally substituted lower alkyl, cycloalkyl, lower alkoxy, hydroxy, optionally substituted aryl, optionally substituted arylalkyl; optionally substituted arylalkyloxy, heterocyclic ring or N-protecting groups, which comprises reacting a compound of the formula I: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above and X is lower alkoxy or halogen with a compound of the formula II: ##STR3## wherein Y, --A--, --B-- and R are as defined above in the presence of a base.
摘要翻译：描述了用于制备式III的立体异构亚苄基衍生物的选择性和高产率方法：其中R 1和R 2各自独立地为低级烷基，低级烷氧基或卤素; Y是SO2，SO或CO; -A-是任选取代的低级亚烷基; -B-是-CH 2 - 或-O-; 或-A-和-B-可以一起形成任选取代的亚苯基或任选取代的低级亚烯基; 并且R是氢，任选取代的低级烷基，环烷基，低级烷氧基，羟基，任选取代的芳基，任选取代的芳基烷基; 任选取代的芳基烷氧基，杂环或N-保护基，其包括使式I化合物：其中R 1和R 2如上所定义，X是低级烷氧基或卤素与式II化合物反应：图像II其中Y，-A-，-B-和R如上所定义，在碱的存在下。

8. 发明授权

US5319100A 3-benzylidene-1-carbamoyl-2-pyrrolidone analogues 失效
标题翻译： 3-亚苄基-1-氨基甲酰基-2-吡咯烷酮类似物
公开(公告)号：US5319100A
公开(公告)日：1994-06-07
申请号：US33342
申请日：1993-03-18
申请人： Susumu Kamata , Takeshi Shiota , Nobuhiro Haga , Toshihiko Okada , Hirokuni Jyoyama , Saichi Matsumoto
发明人： Susumu Kamata , Takeshi Shiota , Nobuhiro Haga , Toshihiko Okada , Hirokuni Jyoyama , Saichi Matsumoto
IPC分类号： C07D207/36 , C07D207/38 , C07D261/12 , C07D263/40 , C07D263/46 , C07D275/02 , C07D275/03 , C07D277/34 , C07D207/12
CPC分类号： C07D275/03 , C07D207/36 , C07D207/38 , C07D261/12 , C07D263/40 , C07D263/46 , C07D277/34
摘要： The present invention relates to novel 3-benzylidene-1-carbamoyl-2-pyrroridone analogues having advantage anti-inflammatory activities, which is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is independently hydrogen, alkyl, alkoxy, or halogen; R.sup.3 is hydrogen or acyl; R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, cyano, or halogen; R.sup.5 and R.sup.6 each is independently hydrogen, alkyl, aryl, aralkyl, heterocyclic group, substituted or unsubstituted amino, or OR.sup.7 wherein R.sup.7 is hydrogen, alkyl, aryl, acyl, or aralkyl, or taken together with the adjacent nitrogen atom may form heterocyclic group which may contain N, O, and/or S, and X and Y each is independently O, S, substituted or unsubstituted imino, or substituted or unsubstituted methylene. In more detail, the present invention provides an anti-inflammatory agent which is useful for the treatment of chronic inflammation and has little side effect, e.g., stomach disease.
摘要翻译：本发明涉及具有抗炎活性优势的新型3-亚苄基-1-氨基甲酰基-2-吡咯酮类似物，其由下式表示：其中R 1和R 2各自独立地为氢，烷基，烷氧基或卤素 ; R3是氢或酰基; R4是氢，烷基，羟基，烷氧基，氰基或卤素; R 5和R 6各自独立地为氢，烷基，芳基，芳烷基，杂环基，取代或未取代的氨基或OR 7，其中R 7为氢，烷基，芳基，酰基或芳烷基，或与相邻氮原子一起形成杂环基其可以含有N，O和/或S，X和Y各自独立地为O，S，取代或未取代的亚氨基，或取代或未取代的亚甲基。更详细地，本发明提供一种抗炎剂，其可用于治疗慢性炎症并且具有很小的副作用，例如胃病。

9. 发明授权

US5043456A 6-oxa and thiabicyclo [3.1.0.] compounds 失效
标题翻译： 6-氧杂和硫杂双环[3.1.0。]化合物
公开(公告)号：US5043456A
公开(公告)日：1991-08-27
申请号：US516141
申请日：1990-04-27
申请人： Mitsuaki Ohtani , Fumihiko Watanabe , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
发明人： Mitsuaki Ohtani , Fumihiko Watanabe , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
IPC分类号： C07D493/08 , A61K31/00 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/557 , A61P7/02 , A61P9/08 , A61P11/08 , C07C20060101 , C07C67/00 , C07C301/00 , C07C311/00 , C07C311/02 , C07C311/07 , C07C311/10 , C07C311/13 , C07C311/15 , C07C311/20 , C07C311/37 , C07C313/00 , C07C323/52 , C07D209/52 , C07D209/56 , C07D213/34 , C07D213/71 , C07D221/22 , C07D303/40 , C07D303/46 , C07D331/02 , C07D491/044 , C07D493/04 , C07D495/04
CPC分类号： C07D493/08 , C07D213/34 , Y02P20/55
摘要： There are provided compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen or C.sub.1 -C.sub.5 alkyl; R.sub.2 is an C.sub.1 -C.sub.10 alkyl, aryl, aralkyl, or pyridyl, where the aryl, aralkyl, or pyridyl are unsubstituted or are substituted by C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, nitro, hydroxy, carboxy, amino, C.sub.1 -C.sub.5 alkylamino, C.sub.1 -C.sub.5 dialkyamino whose two alkyl groups may be different from each other, C.sub.2 -C.sub.3 alkanoylamino, or halogen and X is an C.sub.1 -C.sub.7 alkylene, C.sub.2 -C.sub.7 alkenylene, --CH(F)CH.dbd.CH(CH.sub.2).sub.3 --, --(CH.sub.2).sub.3 --S--(CH.sub.2).sub.2 --, --(CH.sub.2).sub.2 --S--(CH.sub.2).sub.3 --, --C.sub.6 H.sub.4 -O--CH.sub.2 -- or --CH.sub.2 CH.dbd.CH--m--C.sub.6 H.sub.4 --, or their pharmaceutically accepatble salts. The compounds are useful as antithrombotic, anti-vasconstricting and anti-bronchoconstricting drugs.

10. 发明授权

US4605738A Production of 1-phthalidyl-5-fluorouracil derivatives 失效
标题翻译： 1-酞基-5-氟尿嘧啶衍生物的制备
公开(公告)号：US4605738A
公开(公告)日：1986-08-12
申请号：US550219
申请日：1983-11-09
申请人： Susumu Kamata , Nobuhiro Haga , Wataru Nagata , Takeaki Matsui
发明人： Susumu Kamata , Nobuhiro Haga , Wataru Nagata , Takeaki Matsui
IPC分类号： C07D307/90 , C07D405/04 , C07F7/18 , C07D239/10 , C07D307/83
CPC分类号： C07D405/04 , C07D307/90 , C07F7/1856
摘要： Highly selective and high yield process for producing antitumor agent 1-phthalidyl-5-fluorouracil derivatives of formula (I) which comprises reacting a phthalidyl compound (II) with an amine (III) to yield the quaternary ammonium salts (IV), and reacting the latter with 5-fluorouracil. ##STR1## [wherein X is leaving group; ##STR2## is triethylamine, N-methylmorpholine, N-ethylmorpholine, and the like; R.sup.4 and R.sup.5 each is hydrogen, trialkylsilyloxy, alkoxy, nitro, cyano, carboxy, or alkoxycarbonyl].
摘要翻译：用于制备式（I）的抗癌剂1-邻苯二甲酰基-5-氟尿嘧啶衍生物的高选择性和高产率方法，其包括使邻苯二甲酰化合物（II）与胺（III）反应以产生季铵盐（IV），并使后者与5-氟尿嘧啶。 + TR [其中X是离开组; 三乙胺，N-甲基吗啉，N-乙基吗啉等; R 4和R 5各自为氢，三烷基甲硅烷氧基，烷氧基，硝基，氰基，羧基或烷氧基羰基。

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