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1. 发明授权

US5292891A Optically active 2,2-dimethyl-1,3-dioxin-4-ones and method for preparing same and method for preparing optically active compound for synthesis of physiologically active substance and optically active intermediate compound 失效
标题翻译：光学活性的2,2-二甲基-1,3-二恶英-4-酮及其制备方法以及制备用于合成生理活性物质和光学活性中间体化合物的光学活性化合物的方法
公开(公告)号：US5292891A
公开(公告)日：1994-03-08
申请号：US991551
申请日：1992-12-15
申请人： Chikara Kaneko , Masayuki Sato
发明人： Chikara Kaneko , Masayuki Sato
IPC分类号： C07D301/27 , C07D303/42 , C07D309/30 , C07D309/36 , C07D319/06 , C12P17/06 , C12P41/00 , C07D309/10
CPC分类号： C07D319/06 , C07D303/42 , C07D309/30 , C07D309/36 , C12P17/06 , C12P41/004
摘要： There are provided novel and optically active 2,2-dimethyl-1,3-dioxin-4-ones which are useful as starting materials for physiologically active compounds, functional materials or the like. Provided are optically active 5,6-epoxyhexanoic acid esters and novel optically active 6-substituted tetrahydropyran-2-one derivatives. That is, optically active 6-chloromethyltetrahydropyran-2-one can be synthesized by lactonizing optically active 2,2-dimethyl-6-(3-chloro-2-hydroxypropyl)-1,3-dioxin-4-one to form optically active 6-chloromethyltetrahydropyran-2,4-dione; reacting the thus formed compound with hydrogen in the presence of a catalyst to obtain optically active 6-chloromethyl-4-hydroxytetrahydropyran-2-one; subjecting this compound to a dehydration reaction, thereby obtaining optically active 6-chloromethyldihydropyran-2-one; reacting this compound with hydrogen in the presence of a catalyst to form optically active 6-chloromethyltetrahydropyran-2-one; and then treating this compound under basic conditions to prepare an optically active 5,6-epoxyhexanoic acid ester represented by the formula (6) ##STR1## (wherein the symbol * represents an asymmetric carbon atom, and R is a methyl group or an ethyl group).
摘要翻译：提供了可用作生理活性化合物，功能材料等的起始原料的新型和光学活性的2,2-二甲基-1,3-二恶英-4-酮。提供光学活性的5,6-环氧己酸酯和新的光学活性的6-取代的四氢吡喃-2-酮衍生物。也就是说，光学活性的6-氯甲基四氢吡喃-2-酮可以通过将光学活性的2,2-二甲基-6-（3-氯-2-羟丙基）-1,3-二恶英-4-酮内酯化来形成光学活性的 6-氯甲基四氢吡喃-2,4-二酮; 使这样形成的化合物与氢气在催化剂存在下反应，得到光学活性的6-氯甲基-4-羟基四氢吡喃-2-酮; 使该化合物脱水反应，得到光学活性的6-氯甲基二氢吡喃-2-酮; 在催化剂存在下使该化合物与氢气反应形成光学活性的6-氯甲基四氢吡喃-2-酮; 然后在碱性条件下处理该化合物以制备由式（6）表示的光学活性5,6-环氧己酸酯（*化学结构*）（6）（其中符号*表示不对称碳原子，R为甲基或乙基）。

2. 发明授权

US5256800A Optically active 2,2-dimethyl-1,3-dioxin-4-ones and method for preparing same 失效
标题翻译：光学活性的2,2-二甲基-1,3-二恶英-4-酮及其制备方法
公开(公告)号：US5256800A
公开(公告)日：1993-10-26
申请号：US836425
申请日：1992-02-18
申请人： Chikara Kaneko , Masayuki Sato
发明人： Chikara Kaneko , Masayuki Sato
IPC分类号： C07D319/06 , C12P17/06 , C12P41/00
CPC分类号： C12P17/06 , C07D319/06 , C12P41/004
摘要： There are provided novel and optically active 2,2-dimethyl-1,3-dioxin-4-ones which are useful as starting materials for physiologically active compounds, functional materials or the like. Furthermore, a method for preparing an optically active compound comprises reacting a racemic 1,3-dioxin-4-one with vinylacetate in the presence of lipase to resolve the racemic compound into optically active compound represented by the formula (3) ##STR1## and an optically active compound represented by the formula (4) ##STR2## which is an antipode of the compound represented by the formula (3).

3. 发明授权

US4754029A 3-oxo-2-azabicyclohexane derivatives 失效
标题翻译： 3-氧代-2-氮杂双环己烷衍生物
公开(公告)号：US4754029A
公开(公告)日：1988-06-28
申请号：US844011
申请日：1986-03-26
申请人： Chikara Kaneko , Masayuki Sato , Nobuya Katagiri
发明人： Chikara Kaneko , Masayuki Sato , Nobuya Katagiri
IPC分类号： C07D205/08 , C07D205/12 , C07D213/69 , C07D213/89 , C07D487/04
CPC分类号： C07D205/08 , C07D205/12
摘要： 3-Oxo-2-azabicyclohexane derivatives represented by the general formula: ##STR1## wherein R.sub.1 represents an optically active menthoxy group or an optically active 1-phenylethoxy group when R.sub.2 and R.sub.3 are combined to form a bond; when R.sub.3 is a hydrogen atom, R.sub.1 and R.sub.2 are combined to form an oxo group or, R.sub.2 is a hydrogen atom and R.sub.1 is a hydroxy group or a lower alkanoyloxy group. The 3-oxo-2-azabicyclohexane derivatives are novel compounds useful as intermediates for antibacterial agents.
摘要翻译：其中R 1表示光学活性的薄荷氧基或光学活性的1-苯基乙氧基，当R 2和R 3结合形成键时，其通式如下：当R 3为氢原子时，R 1和R 2结合形成氧代基或R 2为氢原子，R 1为羟基或低级烷酰氧基。 3-氧代-2-氮杂双环己烷衍生物是用作抗细菌剂的中间体的新化合物。

4. 发明授权

US4672132A Process for producing an aldehydelactone 失效
标题翻译：醛内酯的制备方法
公开(公告)号：US4672132A
公开(公告)日：1987-06-09
申请号：US834362
申请日：1986-02-28
申请人： Chikara Kaneko , Masayuki Sato
发明人： Chikara Kaneko , Masayuki Sato
IPC分类号： C07D307/935 , C07D307/93
CPC分类号： C07D307/935
摘要： A process for producing 3-oxo-6-formyl-2-oxabicyclo[3.3.0]-6-octene useful as an intermediate for producing prostaglandins, via a few steps from raw materials which can be relatively easily prepared. The process comprises subjecting 2,2-dimethyl-1,3-dioxin-4-one and cis-2-cyclopenten-1,4-diol to addition reaction in a solvent, preferably under a photo-irradiation, removing the solvent from the reaction mixture, adding water to the resulting adducts and reacting the resulting mixture on heating.
摘要翻译：通过可以相对容易制备的原料的几步，制备可用作制备前列腺素的中间体的3-氧代-6-甲酰基-2-氧杂双环[3.3.0] -6-辛烯的方法。该方法包括在溶剂中优选在光照射下将2,2-二甲基-1,3-二恶英-4-酮和顺式-2-环戊烯-1,4-二醇进行加成反应，从溶剂中除去溶剂反应混合物，向所得加合物中加入水，并在加热时使所得混合物反应。

5. 发明授权

US4612379A Process for producing 1,3-dioxin-4-one derivatives 失效
标题翻译： 1,3-二恶英-4-酮衍生物的制备方法
公开(公告)号：US4612379A
公开(公告)日：1986-09-16
申请号：US749426
申请日：1985-06-27
申请人： Chikara Kaneko , Masayuki Sato , Hiromichi Ogasawara
发明人： Chikara Kaneko , Masayuki Sato , Hiromichi Ogasawara
IPC分类号： C07D319/06
CPC分类号： C07D319/06
摘要： A process for producing 1,3-dioxin-4-one derivatives having a lower alkyl group at 2-position and useful as a starting raw material for prostaglandins, with a high yield is provided, which process comprises reacting formyl Meldrum's acid with a lower aliphatic carbonyl compound of 2 to 4 carbon atoms in a solvent containing the carbonyl compound at 100.degree. to 120.degree. C., while portionwise adding the acid into the solvent, the total quantity of the acid added being 0.2 mol or less per liter of the solvent.
摘要翻译：提供了一种生产2-位具有低级烷基并可用作前列腺素起始原料的1,3-二恶英-4-酮衍生物的方法，该方法以高产率生产，该方法包括使甲酰基米糠酸与较低的在含有羰基化合物的溶剂中，在100-120℃下含有2至4个碳原子的脂族羰基化合物，同时将酸加入到溶剂中，加入的酸的总量为每升0.2mol 溶剂。

6. 发明授权

US06482957B2 Cyclopentenecarboxamide derivative, method for preparing the same and bicycloamide derivative used therein 失效
标题翻译：环戊烯酰胺衍生物，其制备方法及其中所用的双环酰胺衍生物
公开(公告)号：US06482957B2
公开(公告)日：2002-11-19
申请号：US10131244
申请日：2002-04-25
申请人： Nobuya Katagiri , Chikara Kaneko , Junko Sato , Masahiro Torihara , Koichi Kanehira , Yoshin Tamai
发明人： Nobuya Katagiri , Chikara Kaneko , Junko Sato , Masahiro Torihara , Koichi Kanehira , Yoshin Tamai
IPC分类号： C07D20952
CPC分类号： C07F9/65616 , C07D209/52 , C07D473/40 , C07F9/5728
摘要： A cyclopentenecarboxamide derivative represented by the formula (I): and a method for preparing the cyclopentencarboxamide derivative. A bicycloamide derivative represented by the formula (II): and a method for preparing the bicycloamide derivative.
摘要翻译：由式（I）表示的环戊烯甲酰胺衍生物及其制备环戊烷羧酰胺衍生物的方法。由式（II）表示的双环酰胺衍生物及其制备双环酰胺衍生物的方法。

7. 发明授权

US4022768A Process for preparation of 1.alpha.,25-dihydroxycholecalciferol 失效
标题翻译：制备1 {60,25-二羟基胆钙化甾醇的方法
公开(公告)号：US4022768A
公开(公告)日：1977-05-10
申请号：US657375
申请日：1976-02-12
申请人： Isao Matsunaga , Kiyoshige Ochi , Hiroyuki Nagano , Minoru Shindo , Masayuki Ishikawa , Chikara Kaneko , Hector F. DeLuca
发明人： Isao Matsunaga , Kiyoshige Ochi , Hiroyuki Nagano , Minoru Shindo , Masayuki Ishikawa , Chikara Kaneko , Hector F. DeLuca
IPC分类号： C07J9/00 , C07J71/00
CPC分类号： C07J71/0042 , C07J9/00
摘要： 1.alpha.,25-dihydroxycholecalciferol is prepared by reacting 1,5,7-trien-3.beta.,25-diol with a 1,2,4-triazoline-dione derivative represented by the formula: ##STR1## wherein R represents an alkyl group or an aryl or substituted-aryl group; reacting the resulting 1,4-cyclic adduct represented by the general formula ##STR2## wherein R is as defined above, with a peroxide to form a 1.alpha.,2.alpha.-epoxide compound represented by the general formula ##STR3## wherein R is as defined above, reducing the so formed compound with a metal hydride to form cholesta-5,7-diene-1.alpha.,3.beta.,25-triol, irradiating the so formed compound with ultraviolet rays to form 1.alpha.,25-dihydroxyprevitamin D.sub.3, isomerizing the so formed previtamin D.sub.3, and recovering 1.alpha.,25-dihydroxycholecalciferol.
摘要翻译： 1α，25-二羟基胆钙化醇通过使1,5,7-三烯-3β，25-二醇与下式表示的1,2,4-三唑啉二酮衍生物反应制备：其中R表示烷基或芳基或取代的芳基; 使得到的由通式“IMAGE”表示的所得1,4-环加成物与上述定义相同，与过氧化物反应，形成由通式“IMAGE”表示的1α，2α-环氧化合物，其中R为用金属氢化物还原形成的化合物以形成胆甾烯-5,7-二烯-1α，3β，25-三醇，用紫外线照射所形成的化合物以形成1α，25-二羟维生素D3，异构化所形成的维生素D3，并回收1α，25-二羟基胆钙化甾醇。

8. 发明授权

US5817812A Cyclopentenecarboxamide derivative, method for preparing the same and bicycloamide derivative used therein 失效
标题翻译：环戊烯酰胺衍生物，其制备方法及其中所用的双环酰胺衍生物
公开(公告)号：US5817812A
公开(公告)日：1998-10-06
申请号：US748981
申请日：1996-11-14
申请人： Nobuya Katagiri , Chikara Kaneko , Junko Sato , Masahiro Torihara , Koichi Kanehira , Yoshin Tamai
发明人： Nobuya Katagiri , Chikara Kaneko , Junko Sato , Masahiro Torihara , Koichi Kanehira , Yoshin Tamai
IPC分类号： C07D209/52 , C07D473/40 , C07F9/572 , C07F9/6561 , C07D473/00 , C07D473/18 , C07D473/26
CPC分类号： C07F9/65616 , C07D209/52 , C07D473/40 , C07F9/5728
摘要： A cyclopentenecarboxamide derivative represented by the formula (I): ##STR1## and a method for preparing the cyclopentencarboxamide derivative. A bicycloamide derivative represented by the formula (II): ##STR2## and a method for preparing the bicycloamide derivative.
摘要翻译：由式（I）表示的环戊烯甲酰胺衍生物：（I）和制备环戊烷羧酰胺衍生物的方法。由式（II）表示的双环酰胺衍生物：＆lt; IMAGE＆gt;（II）和制备双环酰胺衍生物的方法。

9. 发明授权

US5202459A Process for producing cyclobutane derivative 失效
标题翻译：环丁烷衍生物的制备方法
公开(公告)号：US5202459A
公开(公告)日：1993-04-13
申请号：US598233
申请日：1990-10-16
申请人： Chikara Kaneko , Nobuya Katagiri
发明人： Chikara Kaneko , Nobuya Katagiri
IPC分类号： C07C215/42 , C07C217/52 , C07C229/48 , C07C271/24 , C07D205/12
CPC分类号： C07D205/12 , C07C215/42 , C07C217/52 , C07C229/48 , C07C271/24 , C07C2101/04
摘要： The present invention relates to a process for producing cyclobutane derivatives represented by general formula (28): ##STR1## (wherein R represents a substituent; R.sub.2 represents an electron attracting group and Nu represents a substituent corresponding to nucleophilic reagent), by reacting a compound represented by general formula (27): ##STR2## (wherein R has the same significance as defined above and R.sub.1 represents an electron attracting group) with nucleophilic reagents Nu.sup..crclbar. in a solvent.The compounds of formula (28) are useful as intermediates for synthesis of, for example, 9-[2,3-bis(hydroxymethyl)cyclobutan-1-yl]guanine which is expected to be useful as an antiviral agent.
摘要翻译：本发明涉及通式（28）表示的环丁烷衍生物的制造方法：其中，R表示取代基，R2表示吸电子基团，Nu表示与亲核试剂对应的取代基），由在溶剂中使通式（27）表示的化合物：其中R（具有与上述相同的含义并且R 1表示吸电子基团）与亲核试剂Nu（ - ）反应。式（28）的化合物可用作合成例如9- [2,3-双（羟甲基）环丁烷-1-基]鸟嘌呤的中间体，其预期可用作抗病毒剂。

10. 发明授权

US4145357A Steroid derivatives and process for preparing the same 失效
标题翻译：甾体衍生物及其制备方法
公开(公告)号：US4145357A
公开(公告)日：1979-03-20
申请号：US855362
申请日：1977-11-28
申请人： Kiyoshige Ochi , Isao Matsunaga , Minoru Shindo , Chikara Kaneko
发明人： Kiyoshige Ochi , Isao Matsunaga , Minoru Shindo , Chikara Kaneko
IPC分类号： C07C67/00 , C07C401/00 , C07J9/00 , C07J17/00
CPC分类号： C07J9/00 , C07J17/00
摘要： A steroid derivative represented by the formula ##STR1## wherein R is as defined hereunder and a process for preparing the same are disclosed. The derivative is an intermediate for the production of various useful compounds.

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