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1. 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。

2. 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.

3. 发明授权

US4225524A Steroid derivatives and process for preparing the same 失效
标题翻译：类固醇衍生物及其制备方法
公开(公告)号：US4225524A
公开(公告)日：1980-09-30
申请号：US915988
申请日：1978-06-14
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： C07J9/00
CPC分类号： C07J9/00 , C07J9/005
摘要： Steroid derivatives represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are as defined hereunder which is useful for easily producing a wide variety of active vitamin D, and a process for preparing the same are disclosed.
摘要翻译：由式“IMAGE”表示的类固醇衍生物，其中R1和R2如下文所定义，其可用于容易地生产各种活性维生素D及其制备方法。

4. 发明授权

US4179452A 3.alpha.,6.alpha.-Dihydroxy-5.beta.-cholestan-24-one derivatives and process for preparing the same 失效
标题翻译： 3α，6α-二羟基-5β-胆甾烷二酮-24衍生物及其制备方法
公开(公告)号：US4179452A
公开(公告)日：1979-12-18
申请号：US906866
申请日：1978-05-17
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： C07J9/00 , C07J31/00
CPC分类号： C07J31/006 , C07J9/00 , C07J9/005
摘要： 3.alpha.,6.alpha.-Dihydroxy-5.beta.-cholestan-24-one or its derivative represented by the formula ##STR1## wherein R is as defined hereunder which is a useful intermediate for the production of an active vitamin D, and a process for preparing the compound of the formula are disclosed.
摘要翻译： 3α，6α-二羟基-5β-胆固醇-24-或其衍生物，其由下式定义，其中R如下文所定义，其为生产活性维生素D的有用中间体，以及用于公开了制备式的化合物。

5. 发明授权

US4011250A 1.alpha., 2.alpha.-Dihydroxycholecalciferol and process for preparing the same 失效
标题翻译： 1'，2'-二羟基氧基化合物及其制备方法
公开(公告)号：US4011250A
公开(公告)日：1977-03-08
申请号：US602363
申请日：1975-08-06
申请人： Masayuki Ishikawa , Chikara Kaneko , Satoshi Sasaki , Tatsuo Suda , Sachiko Yamada , Akiko Sugimoto
发明人： Masayuki Ishikawa , Chikara Kaneko , Satoshi Sasaki , Tatsuo Suda , Sachiko Yamada , Akiko Sugimoto
IPC分类号： A61K31/045 , A61K31/59 , A61P3/02 , C07C67/00 , C07C401/00 , C07J9/00 , C07J71/00
CPC分类号： C07J9/00 , C07J71/0042
摘要： 1.alpha.,2.alpha.-Dihydroxycholecaliciferol having improved vitamin D activities and a process for preparing the same are disclosed.

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

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）。

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

US06452004B1 Cyclopentenecarboxamide derivative, method for preparing the same bicycloamide derivative used therein 失效
标题翻译：环戊烯甲酰胺衍生物，其中使用的相同双环酰胺衍生物的制备方法
公开(公告)号：US06452004B1
公开(公告)日：2002-09-17
申请号：US09613200
申请日：2000-07-11
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： C07D47300
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。

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