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31. 发明授权

US5264561A Method of manufacturing 2',3'-dideoxy-2',3'-didehydronucleosides 失效
标题翻译：制备2'，3'-二脱氧-2'，3'-二脱氢核苷的方法
公开(公告)号：US5264561A
公开(公告)日：1993-11-23
申请号：US854843
申请日：1992-03-20
申请人： Takashi Ebata , Hajime Matsushita , Nobuhiro Mizutani , Junji Ohki , Junko Tanaka , Hiromi Kaibara , Kazuo Itoh
发明人： Takashi Ebata , Hajime Matsushita , Nobuhiro Mizutani , Junji Ohki , Junko Tanaka , Hiromi Kaibara , Kazuo Itoh
IPC分类号： C07D405/04 , C07D473/00 , C07D473/18 , C07H19/04 , C07H19/00
CPC分类号： C07H19/04 , Y02P20/55
摘要： The instant invention is drawn to a method for manufacturing 2',3'-dideoxy-2',3'-didehydronucleoside compounds by reacting a ribonucleoside derivative wherein the hydroxyl in the 5'-position of the furanose ring of said ribonucleoside is protected by a silyl protective group, with an acid anhydride such as acetic anhydride in the presence of a catalyst such as hydrous zirconium oxide, and then subjecting the reaction product to decarboxylation. The decarboxylation can be effected by heating the reaction product. This method can be performed in a single step, and requires no reagents which are expensive or chemicals which should be handled with care. Hence, it serves to manufacture 2',3'-dideoxy-2',3'-didehydronucleosides easily at low cost.

32. 发明授权

US5216177A Method of preparing trans-3,4-disubstituted-.gamma.-lactones 失效
标题翻译：制备TRANS-3,4-DISUBSTITUTED-（GAMMA）-LACTONES的方法
公开(公告)号：US5216177A
公开(公告)日：1993-06-01
申请号：US695010
申请日：1991-05-03
申请人： Takashi Ebata , Hajime Matsushita , Hiroshi Kawakami , Koshi Koseki
发明人： Takashi Ebata , Hajime Matsushita , Hiroshi Kawakami , Koshi Koseki
IPC分类号： C07D307/33 , C07D315/00 , C07D493/08
CPC分类号： C07D315/00
摘要： First, levoglucosenone is made to react with methyl lithium in the presence of copper iodide in order to introduce a methyl group into an enone group of levoglucosenone, and to obtain 1,6-anhydro-3,4-dideoxy-4-C-methyl-.beta.-D-erythro-hexopyranose-2-ulose. This methyl compound is oxidized in acetic acid for lactone formation, and (3S,4S)-5-hydroxy-3-methylpentan-4-olide is thus obtained. Further, this lactone is made to react with tosyl chloride in anhydrous pyridine to obtain (3S,4S)-3-methyl-5-tosyloxypentan-4-olide (tosylate). The obtained tosylate is alkylated with n-propyl lithium in the presence of copper iodide to obtain (3S,4R)-3-methyl-4-octanolide. Here, the (3S,4S)-3-methyl-5-tosyloxypentan-4-olide may be treated with potassium carbonate to cleave lactone ring once, thereby obtaining epoxide. After that, the obtained epoxide is alkylated to form lactone ring again to obtain (3S,4R)-3-methyl-4-octanolide.

33. 发明授权

US5210317A Method of producing aldehyde by oxidation of primary alcohol 失效
标题翻译：通过氧化一级酒精生产阿尔代氏菌的方法
公开(公告)号：US5210317A
公开(公告)日：1993-05-11
申请号：US768769
申请日：1991-10-17
申请人： Hideyuki Kuno , Makoto Shibagaki , Kyoko Takahashi , Hajime Matsushita
发明人： Hideyuki Kuno , Makoto Shibagaki , Kyoko Takahashi , Hajime Matsushita
IPC分类号： B01J21/06 , C07C45/29
CPC分类号： B01J21/066 , C07C45/29
摘要： Disclosed is a method of producing an aldehyde in which a primary alcohol is reacted with an oxidizing agent selected from the group consisting of ketone, aldehyde and quinone in the presence of a diluent which does not participate in the reaction, in the presence of a partially dehydrated zirconium hydroxide, so as to oxidize the primary alcohol into its corresponding aldehyde.
摘要翻译： PCT No.PCT / JP91 / 00184 Sec。 371日期1991年10月17日 102（e）日期1991年10月17日PCT 1991年2月15日提交PCT公布。出版物WO91 / 12226 1991年8月22日公开。公开了一种制备醛的方法，其中伯醇在不参与反应的稀释剂的存在下与选自酮，醛和醌的氧化剂反应在部分脱水的氢氧化锆的存在下，将伯醇氧化成其相应的醛。

34. 发明授权

US5112994A Method of producing (S)-4-hydroxymethyl-.gamma.-lactone 失效
标题翻译：制备（S）-4-羟基甲基 - （氨基）-L-酮的方法
公开(公告)号：US5112994A
公开(公告)日：1992-05-12
申请号：US583647
申请日：1990-09-17
申请人： Koshi Koseki , Takashi Ebata , Hiroshi Kawakami , Hajime Matsushita , Kazuo Itoh , Yoshitake Naoi
发明人： Koshi Koseki , Takashi Ebata , Hiroshi Kawakami , Hajime Matsushita , Kazuo Itoh , Yoshitake Naoi
IPC分类号： C07D307/33 , C07D493/08
CPC分类号： C07D307/33 , C07D493/08
摘要： (S)-4-hydroxymethyl-.gamma.-lactone is prepared by oxidizing dihydrolevoglucosenone with a peracid in an organic solvent. (S)-4-hydroxymethyl-.gamma.-lactone is prepared from levoglucosenone. First, levoglucosenone is catalytic hydrogenated, thereby dihydrolevoglucosenone is obtained. Next, dihydrolevoglucosenone thus obtained is oxidized with a peracid in an organic solvent, thereby (S)-4-hydroxymethyl-.gamma.-lactone is obtained. In this manner, (S)-4-hydroxymethyl-.gamma.-lactone can be obtained with high optical purity.

35. 发明授权

US4871858A Method of producing formamide compounds 失效
标题翻译：甲酰胺化合物的生产方法
公开(公告)号：US4871858A
公开(公告)日：1989-10-03
申请号：US129663
申请日：1987-12-07
申请人： Hajime Matsushita , Makoto Shibagaki , Kyoko Takahashi
发明人： Hajime Matsushita , Makoto Shibagaki , Kyoko Takahashi
IPC分类号： C07D295/18 , B01J21/04 , B01J21/06 , B01J21/08 , B01J21/12 , B01J29/06 , C07B31/00 , C07B43/06 , C07B61/00 , C07C67/00 , C07C231/00 , C07C231/08 , C07C231/10 , C07C233/02 , C07C233/03 , C07C233/58 , C07C233/65 , C07D295/182 , C07D401/04
CPC分类号： C07D295/182 , C07D401/04
摘要： An amine is reached with dimethyformamioe in the presence of a solid catalyst to produce a formamide corresponding to the amine. The solid catalyst includes an oxide of metals belonging to Groups III, IV and V of the Periodic Table.

36. 发明授权

US4847424A Method of producing aldehyde compound 失效
标题翻译：生产醛化合物的方法
公开(公告)号：US4847424A
公开(公告)日：1989-07-11
申请号：US160156
申请日：1988-02-25
申请人： Hajime Matsushita , Makoto Shibagaki , Kyoko Takahashi
发明人： Hajime Matsushita , Makoto Shibagaki , Kyoko Takahashi
IPC分类号： B01J21/06 , B01J23/14 , C07B61/00 , C07C45/00 , C07C45/41 , C07C47/02 , C07C47/28 , C07C47/52 , C07C67/00
CPC分类号： B01J21/066 , C07C45/41
摘要： A carboxylic acid or its ester is reduced by formic acid in the presence of a hydrous metal oxide solid catalyst, to produce a corresponding aldehyde. Using this method, no harmful waste is by-produced, an aldehyde compound can be produced at relatively low cost, and the aldehyde produced can be easily recovered.

37. 发明授权

US4812909A Cell classification apparatus capable of displaying a scene obtained by superimposing a character scene and graphic scene on a CRT 失效
标题翻译：能够显示通过将字符场景和图形场景叠加在CRT上而获得的场景的细胞分类装置
公开(公告)号：US4812909A
公开(公告)日：1989-03-14
申请号：US79959
申请日：1987-07-31
申请人： Toshiaki Yokobayashi , Ryohei Yabe , Hajime Matsushita
发明人： Toshiaki Yokobayashi , Ryohei Yabe , Hajime Matsushita
IPC分类号： G09G5/40 , G09G1/00 , G09G5/377 , H04N5/265 , H04N5/278 , H04N5/272 , H04N5/262
CPC分类号： H04N5/278
摘要： A first video signal is obtained by picking up an image of a sample by a TV camera. A second video signal representing character information regarding the sample is derived from a memory connected to a computer system. The first and second signals are superposed to obtain a sum signal representing a combined single scene, and the sum signal is displayed as a visible picture on a display device. Before the step of superposition of the first and second video signals, at least one of the video signals may be multiplied by a weight.
摘要翻译：通过用TV摄像机拾取样本的图像来获得第一视频信号。表示与样本有关的字符信息的第二视频信号是从连接到计算机系统的存储器导出的。叠加第一和第二信号以获得表示组合的单个场景的和信号，并且将和信号作为可见图像显示在显示装置上。在第一和第二视频信号的叠加步骤之前，视频信号中的至少一个可以乘以权重。

38. 发明授权

US5416204A Method for preparing 2'-3'-dideoxy-.beta.-nucleosides using 2,2-dideoxy-di(organothio)-pentofuranose intermediates 失效
标题翻译：使用2,2-二脱氧 - 二（有机硫） - 呋喃糖苷中间体制备2'-3'-二脱氧-β-核苷的方法
公开(公告)号：US5416204A
公开(公告)日：1995-05-16
申请号：US971768
申请日：1993-02-12
申请人： Hiroshi Kawakami , Katsuya Matsumoto , Koshi Koseki , Takashi Ebata , Hajime Matsushita , Kazuo Itoh , Yoshitake Naoi
发明人： Hiroshi Kawakami , Katsuya Matsumoto , Koshi Koseki , Takashi Ebata , Hajime Matsushita , Kazuo Itoh , Yoshitake Naoi
IPC分类号： C07D405/04 , C07F7/18 , C07H19/06 , C07H19/073 , C07H1/00
CPC分类号： C07D405/04 , C07F7/1856 , C07H19/06 , Y02P20/55
摘要： 2,3-Dideoxy-2,2-di(organothio)-B-D-pentofuranosyl-pyrimidines are disclosed as intermediates in the synthesis of 2', 3'-dideoxynucleosides and have the structure shown below. ##STR1## wherein R.sup.4 is a hydroxyl protecting group;X is oxygen or nitrogen, said nitrogen being bonded to a hydrogen atom, an alkyl or acyl group;Y is hydrogen, halogen, alkyl, haloalkyl or haloalkenyl; andR.sup.5 is alkyl, aralkyl, or aryl wherein aralkkyl or aryl is substituted with hydrogen, halogen, nitro or alkoxy.2', 3'-Dideoxynucleosides, products of the above intermediates, are useful as antiviral agents.
摘要翻译： PCT No.PCT / JP92 / 00752 Sec。 371日期：1993年2月12日 102（e）日期1993年2月12日PCT提交1992年6月12日PCT公布。公开号WO92 / 22548 1992年12月23日的日期.2,3-二脱氧-2,2-二（有机硫）-B-D-呋喃鸟糖基 - 嘧啶作为2'，3'-双脱氧核苷合成中的中间体被公开，具有如下结构。其中R 4是羟基保护基; X是氧或氮，所说的氮键合到氢原子，烷基或酰基上; Y是氢，卤素，烷基，卤代烷基或卤代烯基; R 5为烷基，芳烷基或芳基，其中芳烷基或芳基被氢，卤素，硝基或烷氧基取代。 2'，3'-双脱氧核苷，上述中间体的产物可用作抗病毒剂。

39. 发明授权

US5412111A Method of preparing (3R,4R)-3-hydroxy-4-hydroxymethyl-4-butanolide 失效
标题翻译：制备（3R，4R）-3-羟基-4-羟甲基-4-丁醇酯的方法
公开(公告)号：US5412111A
公开(公告)日：1995-05-02
申请号：US095182
申请日：1993-07-23
申请人： Katsuya Matsumoto , Takashi Ebata , Koshi Koseki , Koji Okano , Hiroshi Kawakami , Hajime Matsushita
发明人： Katsuya Matsumoto , Takashi Ebata , Koshi Koseki , Koji Okano , Hiroshi Kawakami , Hajime Matsushita
IPC分类号： C07D307/33 , C07D493/04 , C07D493/08 , C07D493/18 , C07H3/10
CPC分类号： C07D307/33 , C07D493/08 , C07H3/10
摘要： Providing a method of preparing (3R,4R)-3-hydroxy-4-hydroxymethyl-4-butanolide conveniently and selectively from a widely available raw material in a high yield. A carbonyl group of the 2-position of levoglucosenone is reduced to obtain a hydroxyl group of a .beta.-configuration. Then, an iodo-group of an .alpha.-configuration and an acyloxy ion of a .beta.-configuration are introduced regioselectively and stereoselectively to the double bond at the 4-position and the 3-position of the above-mentioned levoglucosenone, respectively, keeping a trans stereochemical relationship. An alkoxide is then formed, by hydrolysis and an oxirane ring of a .beta.-configuration is formed by removing an iodo-group by intramolecular nucleophilic displacement reaction of the alkoxide. After the hydroxyl group of the 2-position is oxidized to convert to a carbonyl group, the oxirane ring is reductively and selectively cleaved, thereby obtaining a chemical compound having no substituent at the 3-position and a hydroxyl group of a .beta.-configuration at the 4-position. Finally a lactone of 5-membered-ring is prepared by subjecting the above-obtained compound to Baeyer-Villigar oxidation.
摘要翻译：提供从广泛获得的原料中以高产率方便且有选择地制备（3R，4R）-3-羟基-4-羟甲基-4-丁醇的方法。缩合左旋葡萄糖酮的2-位的羰基，得到β-构型的羟基。然后，分别对上述左旋葡萄糖酮的4-位和3-位分别选择性且立体选择地引入α-构型的碘组和β-构型的酰氧基，保持反式立体化学关系。然后通过水解形成醇盐，通过醇盐的分子内亲核取代反应除去碘基形成β-构型的环氧乙烷环。在2-位的羟基被氧化转化成羰基之后，环氧乙烷环被还原和选择性地裂解，从而得到在3-位没有取代基的化合物和β-构型的羟基在 4位。最后通过将上述得到的化合物进行Baeyer-Villigar氧化来制备5元环的内酯。

40. 发明授权

US5410038A method of preparing D-altrose 失效
标题翻译：制备D-阿托糖的方法
公开(公告)号：US5410038A
公开(公告)日：1995-04-25
申请号：US849387
申请日：1992-05-12
申请人： Katsuya Matsumoto , Takashi Ebata , Hajime Matsushita
发明人： Katsuya Matsumoto , Takashi Ebata , Hajime Matsushita
IPC分类号： C07H3/02 , C07H3/10 , C07H1/00
CPC分类号： C07H3/10 , C07H3/02
摘要： Disclosed is a method of preparing D-altrose (4) from the starting material levo-glucosenon (1) in accordance with reactions denoted by reaction formulas (I), (II) and (III) given below: ##STR1##
摘要翻译： PCT No.PCT / JP91 / 01376 Sec。 371日期：1992年5月12日 102（e）日期1992年5月12日PCT 1991年10月9日PCT公布。出版物WO92 / 06986 日期：1992年4月3日。公开是根据由下列给出的反应式（I），（II）和（III）表示的反应从原料左旋葡萄糖酮（1）制备D-麦芽糖（4）的方法（图）（三）（三）

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