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1. 发明授权

US4501700A Preparation of optically active 4-demethoxydaunomycinone 失效
标题翻译：光学活性4-脱甲氧基多霉素酮的制备
公开(公告)号：US4501700A
公开(公告)日：1985-02-26
申请号：US471354
申请日：1983-03-02
申请人： Shiro Terashima , Katsumi Tamoto , Kenji Koga
发明人： Shiro Terashima , Katsumi Tamoto , Kenji Koga
IPC分类号： C07C45/67 , C07C43/178 , C07C45/00 , C07C46/00 , C07C49/577 , C07C50/38 , C07C67/00 , C07C50/36
CPC分类号： C07C43/1786
摘要： A process for preparing racemic 4-demethoxy-7-deoxydaunomycinone which comprises methylating an optically active .alpha.-hydroxyketone to give the corresponding methylated product of either one of the formulas: ##STR1## and reacting the latter with an acid to give a racemate of the .alpha.-hydroxyketone of the formula: ##STR2## .
摘要翻译：一种制备外消旋4-脱甲氧基-7-脱氧果香霉素酮的方法，其包括使光学活性的α-羟基酮甲基化，得到下式之一的相应的甲基化产物：（VI）和（VIB），并使后者与酸反应，得到下式的α-羟基酮的外消旋物：（I）。

2. 发明授权

US4495103A Preparation of optically active 4-demethoxydaunomycinone 失效
标题翻译：光学活性4-脱甲氧基多霉素酮的制备
公开(公告)号：US4495103A
公开(公告)日：1985-01-22
申请号：US471338
申请日：1983-03-02
申请人： Shiro Terashima , Katsumi Tamoto , Masamichi Sugimori
发明人： Shiro Terashima , Katsumi Tamoto , Masamichi Sugimori
IPC分类号： C07C43/178 , C07C50/36 , C07C167/02
CPC分类号： C07C43/1786
摘要： A process for preparing optically active 4-demethoxy-7-deoxydaunomycinone which comprises reacting a racemic mixture of the .alpha.-hydroxyketone of the formula: ##STR1## with an optical isomer of the .alpha.-glycol of the formula: ##STR2## wherein R is a group of the formula: ##STR3## and X is a halogen atom or a lower alkyl group to give a diastereomeric mixture of the acetal of the formula: ##STR4## .
摘要翻译：一种制备光学活性4-脱甲氧基-7-脱氧果香霉素酮的方法，其包括将下式的α-羟基酮的外消旋混合物与下式的α-二醇的旋光异构体反应：（II）其中R是下式的基团：其中X是卤素原子或低级烷基，得到下式的缩醛的非对映体混合物：（III）。

3. 发明授权

US5231179A Heterocyclic compounds and their production 失效
标题翻译：杂环化合物及其生产
公开(公告)号：US5231179A
公开(公告)日：1993-07-27
申请号：US684488
申请日：1991-04-12
申请人： Shiro Terashima , Yoshio Ito , Takeo Kawabata , Kunikazu Sakai , Tamejiro Hiyama , Yoshikazu Kimura , Makoto Sunagawa , Katsumi Tamoto , Akira Sasaki
发明人： Shiro Terashima , Yoshio Ito , Takeo Kawabata , Kunikazu Sakai , Tamejiro Hiyama , Yoshikazu Kimura , Makoto Sunagawa , Katsumi Tamoto , Akira Sasaki
IPC分类号： C07D205/08 , C07D233/32 , C07D263/26 , C07D263/52 , C07D263/58 , C07D403/06 , C07D413/06
CPC分类号： C07D263/52 , C07D205/08 , C07D233/32 , C07D263/26 , C07D263/58 , C07D403/06 , C07D413/06
摘要： A compound of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a hydrogen atom, a lower alkyl group, an ar(lower)alkyl group or an aryl group, or R.sub.1 and R.sub.2 may be combined together to form a lower alkylene group and/or R.sub.3 and R.sub.4 are combined together to form a lower alkylene group, or R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be combined together to form an o-phenylene group, X is a halogen atom and Y is an oxygen atom or a nitrogen atom substituted with lower alkyl or aryl, which is useful as an intermediate in the synthesis of 1.beta.-methylcarbapenem compounds valuable as antibiotics.
摘要翻译：下式的化合物：其中R 1，R 2，R 3和R 4各自为氢原子，低级烷基，芳（低级）烷基或芳基，或者R 1和R 2可以组合一起形成低级亚烷基和/或R 3和R 4结合在一起形成低级亚烷基，或者，R 1，R 2，R 3和R 4可以组合在一起形成邻亚苯基，X是卤素原子，Y 是氧原子或被低级烷基或芳基取代的氮原子，其可用作合成作为抗生素有价值的1β-甲基碳青霉烯化合物的中间体。

4. 发明授权

US4212828A Novel process for asymmetric synthesis of optically active 2-alkanoyl-1,2,3,4-tetrahydro-2-naphthol compounds 失效
标题翻译：光学活性2-烷酰基-1,2,3,4-四氢-2-萘酚化合物不对称合成的新方法
公开(公告)号：US4212828A
公开(公告)日：1980-07-15
申请号：US963174
申请日：1978-11-24
申请人： Kenji Koga , Shiro Terashima
发明人： Kenji Koga , Shiro Terashima
IPC分类号： C07C49/573 , C07C45/00 , C07C45/45 , C07C51/00 , C07C51/06 , C07C62/32 , C07C62/34 , C07C67/00 , C07D207/16 , C07D498/04 , C07D498/10 , C07C65/14
CPC分类号： C07C62/32 , C07C45/45 , C07C62/34 , C07D207/16
摘要： A process for asymmetric synthesis of optically active 2-alkanoyl-1,2,3,4-tetrahydro-2-naphthol compounds of the formula: ##STR1## from L-proline or its ester and the following carboxylic acid of the formula: ##STR2## or its reactive derivative through the following intermediary compounds in order: ##STR3##
摘要翻译：由L-脯氨酸或其酯和下式的下列羧酸不对称合成下式的光学活性2-烷酰基-1,2,3,4-四氢-2-萘酚化合物的方法： IMAGE>或其反应性衍生物通过以下中间体化合物按顺序：和

5. 发明授权

US4338255A Modified lithium aluminum hydrides 失效
标题翻译：改性锂铝氢化物
公开(公告)号：US4338255A
公开(公告)日：1982-07-06
申请号：US238136
申请日：1981-02-25
申请人： Shiro Terashima , Norihiko Tanno , Kenji Koga
发明人： Shiro Terashima , Norihiko Tanno , Kenji Koga
IPC分类号： C07C43/23 , C07F5/06
CPC分类号： C07C43/23 , C07F5/069
摘要： Novel modified lithium aluminum hydride type reducing agents obtained by reacting one equivalent of lithium aluminum hydride with one equivalent of an optically active N-substituted ephedrine of the formula, ##STR1## (wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl group or benzyl group, and Ph is phenyl group)and two equivalents of an N-substituted aniline of the formula, ##STR2## (wherein R.sub.2 is C.sub.1 -C.sub.4 alkyl group or phenyl group, and Ph is phenyl group).This reducing agent is usable for reducing the organic compounds having a carbonyl group (ketone group or aldehyde group) in their structure into the corresponding alcohols. It is particularly useful as a reducing agent for asymmetrically reducing the unsymmetrical ketones to selectively produce either an alcohol in which the asymmetric carbon atom bonded to the hydroxy group is in R-configuration or an alcohol in which said asymmetric carbon atom is in S-configuration.
摘要翻译：通过使一当量氢化铝锂与1当量的下式的光学活性N-取代麻黄碱（其中R1是C1-C4烷基或苄基，和 Ph是苯基）和两当量的下式的N-取代的苯胺，其中R 2是C 1 -C 4烷基或苯基，Ph是苯基。该还原剂可用于将其结构中具有羰基（酮基或醛基）的有机化合物还原成相应的醇。作为用于不对称地还原不对称酮以选择性地产生其中与羟基键合的不对称碳原子处于R-构型的醇或其中所述不对称碳原子处于S-构型的醇中的还原剂是特别有用的。

6. 发明授权

US4418218A Process for producing dihydronaphthalene derivatives 失效
标题翻译：二氢萘衍生物的制备方法
公开(公告)号：US4418218A
公开(公告)日：1983-11-29
申请号：US363048
申请日：1982-03-29
申请人： Shiro Terashima , Norihiko Tanno , Kenji Koga
发明人： Shiro Terashima , Norihiko Tanno , Kenji Koga
IPC分类号： C07C43/23 , C07F5/06 , C07C41/18
CPC分类号： C07C43/23 , C07F5/069
摘要： 2-(1'-hydroxy)ethyl-5,8-dimethoxy-3,4-dihydronaphthalene of the formula ##STR1## is produced by reducing 2-acetyl-5,8-dimethoxy-3,4-dihydronaphthalene of the formula, ##STR2## with a reducing agent obtained by reacting one equivalent of lithium aluminum hydride with one equivalent of an optically active N-substituted ephedrine of the formula, ##STR3## (wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl group or benzyl group, and Ph is phenyl group) and two equivalents of an N-substituted aniline of the formula, ##STR4## (wherein R.sub.2 is a C.sub.1 -C.sub.4 alkyl group or phenyl group, and Ph is phenyl group).

7. 发明授权

US6066742A Intermediates for the preparation of duocarmycin SA and derivatives thereof, and process for the production of the intermediates 失效
标题翻译：制备杜卡霉素SA及其衍生物的中间体，以及生产中间体的方法
公开(公告)号：US6066742A
公开(公告)日：2000-05-23
申请号：US254515
申请日：1999-03-09
申请人： Yasumichi Fukuda , Shiro Terashima
发明人： Yasumichi Fukuda , Shiro Terashima
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P35/00 , C07D209/12 , C07D487/04
CPC分类号： C07D487/04 , C07D209/12 , Y02P20/55
摘要： Indole derivatives shown by the formulae (1), (2a) and (2b) ##STR1## (wherein R.sup.1 is a protecting group for amino group; R.sup.2 is a protecting group for hydroxyl group; R.sup.3 is a protecting group for hydroxyl group; R.sup.4 is a C.sub.1 -C.sub.6 linear or branched lower alkyl group, or benzyl group), and pyrroloindole derivatives shown by formula (3) ##STR2## (wherein R.sup.1 is a protecting group for amino group; R.sup.2 is a protecting group for hydroxyl group; R.sup.3 is a protecting group for hydroxyl group; R.sup.4 is a C.sub.1 -C.sub.6 linear or branched lower alkyl group, or benzyl group), both of which are intermediates for duocarmycin SA, which is expected to be used as an anticancer agent, and derivatives thereof; and a method for producing the same.
摘要翻译： PCT No.PCT / JP97 / 02207 Sec。 371日期1999年3月9日 102（e）1999年3月9日PCT提交1997年6月26日PCT公布。第WO98 / 12197号公报日期：1998年3月26日由式（1），（2a）和（2b）表示的衍生物（其中R1是氨基的保护基; R2是羟基的保护基; R3是羟基的保护基 R4为C1-C6直链或支链低级烷基或苄基）和式（3）所示吡咯并吲哚衍生物（其中R1为氨基保护基; R2为羟基保护基; R3为羟基的保护基; R4是C1-C6直链或支链的低级烷基或苄基），它们都是预期用作抗癌剂的杜卡霉素SA的中间体及其衍生物; 及其制造方法。

8. 发明授权

US4564674A Process for an anthracycline derivative, and an anthracyclinone derivative useful for the process 失效
标题翻译：蒽环类衍生物的方法和用于该方法的蒽环类衍生物衍生物
公开(公告)号：US4564674A
公开(公告)日：1986-01-14
申请号：US662833
申请日：1984-10-19
申请人： Shiro Terashima , Yoshikazu Kimura , Michiyo Suzuki , Teruyo Matsumoto , Rumiko Abe
发明人： Shiro Terashima , Yoshikazu Kimura , Michiyo Suzuki , Teruyo Matsumoto , Rumiko Abe
IPC分类号： C07F7/18 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252 , C07F7/1856
摘要： A process for producing an anthracycline derivative represented by the general formula: ##STR1## where R.sup.1 is an acyl group, each of X.sup.1 and X.sup.2 is a hydrogen atom, a methoxy group, a hydroxyl group, a halogen atom or a lower alkyl group, each of Y.sup.1 and Y.sup.2 is a hydrogen atom, an alkoxy group or a hydroxyl group, and Z is a hydrogen atom or a protected hydroxyl group, which comprises reacting an anthracyclinone derivative represented by the general formula: ##STR2## where R is a hydrogen atom or a trialkylsilyl group, and X.sup.1, X.sup.2, Y.sup.1, Y.sup.2 and Z are as defined above, with a 1-acyl-sugar derivative represented by the general formula: ##STR3## where R.sup.2 is an acyl group and R.sup.1 is as defined above, in the presence of a silyl sulfonic acid derivative represented by the general formula:R.sup.5 R.sup.4 R.sup.3 SiOSO.sub.2 A (IV)where each of R.sup.3, R.sup.4 and R.sup.5 is an alkyl group and A is an alkyl group, an aryl group, a polyfluoroalkyl group or a hydrogen atom.
摘要翻译：一种制备由以下通式表示的蒽环衍生物的方法：其中R1是酰基，其中X1和X2分别是氢原子，甲氧基，羟基，卤原子或低级烷基，Y 1和Y 2各自为氢原子，烷氧基或羟基，Z为氢原子或被保护的羟基，其包括使由通式（II）表示的蒽环腈衍生物：）其中R是氢原子或三烷基甲硅烷基，X 1，X 2，Y 1，Y 2和Z如上所定义，与通式如下的1-酰基 - 糖衍生物反应：其中R 2为在通式R5R4R3SiOSO2A（IV）表示的甲硅烷基磺酸衍生物存在下，酰基和R 1如上所定义，其中R3，R4和R5各自为烷基，A为烷基，芳基基团，多氟烷基或氢原子。

9. 发明授权

US6080859A Pyrroloindole derivatives and intermediates in producing the same 失效
标题翻译：吡咯并吲哚衍生物及其制备中间体
公开(公告)号：US6080859A
公开(公告)日：2000-06-27
申请号：US341872
申请日：1999-07-19
申请人： Yasumichi Fukuda , Rumiko Shimazawa , Yasuo Oomori , Shiro Terashima
发明人： Yasumichi Fukuda , Rumiko Shimazawa , Yasuo Oomori , Shiro Terashima
IPC分类号： C07D487/04 , A61K31/5377 , C07D413/14
CPC分类号： C07D487/04
摘要： Pyrroloindole derivatives having antimicrobial and antitumor activities and having a carbamoyloxy group represented by the following general formula (1), optical isomers thereof, and pharmacologically acceptable salts thereof; and intermediates for production thereof: ##STR1## where R.sup.1 is OH, or a pyrrolidinyl group; n is 1 or 2; R.sup.2 is a lower alkyl group of C.sub.1 -C.sub.4 ; X--Y or Y--X is CH.sub.2, CHOH, CH.sub.2 -CH.sub.2, O--CH.sub.2, or NMe--CH.sub.2 ; Z.sup.1 is Cl or Br; and Ar.sup.1 is ##STR2## wherein Z.sup.2 and Z.sup.3 are O or NH; m is 0 or an integer of 1 to 4; and Ar.sup.2 is any of the above groups a, b, c, and d.
摘要翻译： PCT No.PCT / JP98 / 00234 Sec。 371日期1999年7月19日第 102（e）1999年7月19日PCT PCT 1998年1月22日PCT公布。第WO98 / 32757号公报 1998年7月30日具有抗微生物和抗肿瘤活性并具有由以下通式（1）表示的氨基甲酰氧基的吡咯并吲哚衍生物，其旋光异构体及其药理学上可接受的盐; 及其生产中间体：其中R 1为OH或吡咯烷基; n为1或2; R2是C1-C4的低级烷基; X-Y或Y-X是CH 2，CHOH，CH 2 -CH 2，O-CH 2或NMe-CH 2; Z1是Cl或Br; 和Ar1是其中Z2和Z3是O或NH; m为0或1〜4的整数; 并且Ar 2是上述基团a，b，c和d中的任一个。

10. 发明授权

US4849345A L-phenylalanine dehydrogenase and use thereof 失效
标题翻译： L-苯丙氨酸脱氢酶及其用途
公开(公告)号：US4849345A
公开(公告)日：1989-07-18
申请号：US851207
申请日：1986-04-14
申请人： Yasuhisa Asano , Akiko Nakazawa , Shiro Terashima , Kiyosi Kondo , Kaori Endo , Kenji Hirai , Naganori Numao
发明人： Yasuhisa Asano , Akiko Nakazawa , Shiro Terashima , Kiyosi Kondo , Kaori Endo , Kenji Hirai , Naganori Numao
IPC分类号： C12N9/06 , C12P1/00 , C12P13/04
CPC分类号： C12N9/0018 , C12N9/0028 , C12P1/00 , C12P13/04 , Y10S435/822 , Y10S435/832
摘要： New L-phenylalanine dehydrogenases produced by a microorganism belonging to the genus Sporosarcina or Bacillus, new microorganisms capable of l-phenylalanine dehydrogenase and belonging to the genus Sporosarcina or Bacillus, a process for production of L-phenylalanine dehydrogenase using the microorganisms, and processes for production of L-amino acids using the enzymes or the microorganisms.

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