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21. 发明授权

US4078139A Process for deoxygenating secondary alcohols 失效
标题翻译：脱醇仲醇的方法
公开(公告)号：US4078139A
公开(公告)日：1978-03-07
申请号：US704703
申请日：1976-07-12
申请人： Derek H. R. Barton , Stuart W. McCombie
发明人： Derek H. R. Barton , Stuart W. McCombie
IPC分类号： C07C1/22 , C07B31/00 , C07B35/06 , C07B61/00 , C07C1/00 , C07C9/00 , C07C67/00 , C07H1/00 , C07H9/04 , C07H13/12 , C07H15/203 , C07H15/22 , C07H15/234 , C07H15/236 , C07H15/244 , C07J9/00 , C07J31/00 , C07J43/00 , C07J51/00 , C07J75/00
CPC分类号： C07H9/04 , C07C327/00 , C07H13/12 , C07H15/236 , C07J31/006 , C07J43/003 , C07J51/00 , C07J9/00
摘要： The process for removing a secondary hydroxyl group from an organic compound having at least one secondary hydroxyl group and having any amino groups protected, comprises the reaction of a reactive ester of said secondary hydroxyl group selected from the group consisting of an O-alkylthioester and an O-alkylselenoester with at least one mole of an organotin hydride, preferably tri-n-butylstannane, in an inert, aprotic solvent at a temperature of at least about 100.degree. C and under an inert atmosphere.The process is particularly useful in removing secondary alcohols in aminoglycoside antibiotics to produce deoxy derivatives thereof having antibacterial activity.Also described are novel O-sec.-alkylthiobenzoate, O-sec.-alkyl-S-methylxanthate, N-(sec.-alkoxythiocarbonyl)-imidazole esters, and di-O-alkylthiocarbonates having at least one secondary O-alkyl group, useful intermediates of the claimed process.
摘要翻译：从具有至少一个仲羟基并具有任何氨基保护的有机化合物中除去仲羟基的方法包括所述仲羟基的反应性酯选自由O-烷基硫酯和 O-烷基硒酯与至少一摩尔有机锡氢化物，优选三正丁基锡烷在惰性，非质子溶剂中，在至少约100℃的温度和惰性气氛下反应。

22. 发明授权

US4064148A Chemical process for preparing .DELTA.9(11) dehydrosteroids 失效
标题翻译：制备{66 9（11）脱氢甾醇的化学方法
公开(公告)号：US4064148A
公开(公告)日：1977-12-20
申请号：US688714
申请日：1976-05-21
申请人： Derek H. R. Barton , Robert H. Hesse
发明人： Derek H. R. Barton , Robert H. Hesse
IPC分类号： C07J7/00 , C07J5/00 , C07J41/00 , C07J3/00
CPC分类号： C07J41/005 , C07J5/0076
摘要： The Specification describes a synthetic route for the preparation of a 9,11-dehydro-3-oxygenated 17.alpha.-hydroxy-20-ketopregnane which comprises the steps (i) electrophilically fluorinating a saturated 9,11-unsubstituted 3-oxygenated-17.alpha.-(esterified hydroxy)-20-ketopregnane, (ii) dehydrofluorinating the resulting 9.alpha.-fluorosteroid, if desired after transformations elsewhere in the molecule have been effected, and (iii) cleaving the ester group at the 17.alpha.-position to generate a 17.alpha.-hydroxy group.
摘要翻译：该说明书描述了用于制备9,11-脱氢-3-氧化的17α-羟基-20-酮戊二酸的合成路线，其包括步骤（i）亲和氟化饱和9,11-未取代的3-氧化-17α- （酯化羟基）-20-酮戊二醇，（ii）如果需要，在所述分子中其它地方进行转化后，将所得9α-氟类固醇脱氟化氢，和（iii）在17α位置切割酯基以产生 17α-羟基。

23. 发明授权

US5473085A Production of (-)dodecahydro-3a,6,6,9a-tetramethyl-naphtho[2,1-b] furan 失效
标题翻译：（ - ）十二氢-3a,6,9,9-四甲基 - 萘并[2,1-b]呋喃的生产
公开(公告)号：US5473085A
公开(公告)日：1995-12-05
申请号：US314507
申请日：1994-09-28
申请人： Derek H. R. Barton , Dennis K. Taylor , Chi-Lam Tse
发明人： Derek H. R. Barton , Dennis K. Taylor , Chi-Lam Tse
IPC分类号： C07D307/92
CPC分类号： C07D307/92
摘要： Preparation of a methyl ketone intermediate useful in the synthesis of (-)-dodecahydro-3a,6,6, 9a-tetramethyl-naphtho(2,1-b) furan by subjecting (-)-sclareol to ozonolysis in the presence of iodine or iodine-containing compound. The intermediate can be converted to (-)-dodecahydro-3a,6,6,9a-tetramethyl-naphtho(2,1-b) furan by Baeyer-Villiger oxidation followed by reduction of the resulting product in the presence of a Lewis acid.
摘要翻译：（ - ） - 十二氢-3a,6,6,9a-四甲基萘并（2,1-b）呋喃的合成中使用（ - ） - 香紫苏醇在碘存在下进行臭氧分解的甲基酮中间体的制备或含碘化合物。可以通过Baeyer-Villiger氧化将中间体转化为（ - ） - 十二氢-3a，6,6,9a-四甲基萘并（2,1-b）呋喃，然后在路易斯酸存在下还原所得产物。

24. 发明授权

US5463089A Preparation of ambrox 失效
标题翻译：制备电解质
公开(公告)号：US5463089A
公开(公告)日：1995-10-31
申请号：US279160
申请日：1994-07-22
申请人： Derek H. R. Barton , Shyamal I. Parekh , Dennis K. Taylor , Chi-lam Tse
发明人： Derek H. R. Barton , Shyamal I. Parekh , Dennis K. Taylor , Chi-lam Tse
IPC分类号： C07D307/92
CPC分类号： C07D307/92
摘要： Synthesis of (-)-dodecahydro-3a,6,6,9a-tetramethyl-naphtho(2,1-b)furan from sclareol in a three-stage process.
摘要翻译：在三步法中从香紫苏醇合成（ - ） - 十二氢-3a，6,6,9a-四甲基萘并（2,1-b）呋喃。

25. 发明授权

US4490296A Compositions and method 失效
标题翻译：组合和方法
公开(公告)号：US4490296A
公开(公告)日：1984-12-25
申请号：US462684
申请日：1983-01-31
申请人： Derek H. R. Barton , William B. Motherwell , Samir Z. Zard
发明人： Derek H. R. Barton , William B. Motherwell , Samir Z. Zard
IPC分类号： C07B37/04 , B01J31/00 , B01J31/02 , C07B31/00 , C07B61/00 , C07C67/00 , C07C205/04 , C07J5/00 , C07J7/00 , C07J9/00 , C07J13/00 , C07J41/00 , C07J63/00
CPC分类号： C07J13/005 , C07C201/12 , C07J41/0038 , C07J5/0015 , C07C2102/10
摘要： A novel nitromethylation composition comprising nitromethane and a catalytic amount of a bifunctional basic catalyst, optionally in an organic solvent, a method of nitromethylating ketonic compounds with said compositions and novel steroids of the formulae ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted with an oxygen or nitrogen group or halogen and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A,B,C and D rings optionally contain at least one double bond and optionally substituted with at least one member of the group consisting of --OH, .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms and their use to form the corresponding 21-acetoxy-20-ketocorticosteroids compounds in a simple manner.
摘要翻译：一种包含硝基甲烷和催化量的双功能碱性催化剂，任选在有机溶剂中的新型硝基甲基化组合物，具有所述组合物的酮化合物的硝基甲基化方法以及式I和I'的新类固醇，其中R1是选自氢，任选被氧或氮基团取代的1至4个碳原子的烷基或2至4个碳原子的链烯基和炔基，R 2是1至4个碳原子的烷基，A，B C和D环任选地含有至少一个双键并任选被至少一个由以下组成的组取代：-OH，= 0，卤素，具有1至4个碳原子的烷基和烷氧基，以及2至4个的烯基和炔基碳原子和它们用于以简单的方式形成相应的21-乙酰氧基-20-酮皮质类固醇化合物。

26. 发明授权

US4468494A Polymeric pH-sensitive optical filter agents having hydrazone moieties attached thereto 失效
标题翻译：具有连接有腙部分的聚合物pH敏感光学滤光剂
公开(公告)号：US4468494A
公开(公告)日：1984-08-28
申请号：US250401
申请日：1981-04-02
申请人： Derek H. R. Barton , Irena Y. Bronstein-Bonte , Lloyd D. Taylor
发明人： Derek H. R. Barton , Irena Y. Bronstein-Bonte , Lloyd D. Taylor
IPC分类号： G03C8/48 , C08F8/34 , C08F8/30
CPC分类号： G03C8/48
摘要： Polymeric optical filter agents and photographic products and processes using same are disclosed. The polymeric optical filter agents are pH-sensitive optical filter agents comprising polymeric backbone units having the following hydrazone moiety: ##STR1## where R is a group which can provide a double bond for conjugation with the ##STR2## portion of the moiety to provide light-absorbing capability for the agent at a pH above its pKa, and X represents a substituent of R providing at least one electron-withdrawing group. The polymeric pH-sensitive optical filter agents have a highly colored light-absorbing form at a pH above the pKa and are substantially non-absorbing at a pH below the pKa. The polymeric optical filter agents are useful in photographic film units and processes for the protection of photoexposed photosenstive elements against the occurence of fogging during in-light development.
摘要翻译：公开了聚合物光学滤光剂和使用它们的照相产品和方法。聚合物光学过滤剂是pH敏感的光学过滤剂，其包含具有以下腙部分的聚合物主链单元：其中R是能够提供双键以与该部分的“IMAGE”部分缀合以提供光的基团 - 在高于其pKa的pH下的试剂的吸收能力，X表示提供至少一个吸电子基团的R的取代基。聚合物pH敏感光学过滤剂在高于pKa的pH下具有高度着色的光吸收形式，并且在低于pKa的pH下基本上不吸收。聚合物光学滤光剂可用于照相胶片单元和用于保护光敏光敏元件免于在光照显影过程中发生雾化的过程。

27. 发明授权

US4434080A Dehydrogenation agents based on derivatives of selenium and their use in the dehydrogenation in the 1,4 positions of steroids 失效
标题翻译：基于硒衍生物的脱氢剂及其在类固醇1,4位脱氢中的应用
公开(公告)号：US4434080A
公开(公告)日：1984-02-28
申请号：US379434
申请日：1982-05-18
申请人： Derek H. R. Barton , William B. Motherwell
发明人： Derek H. R. Barton , William B. Motherwell
IPC分类号： C07C45/65 , B01J27/02 , B01J27/057 , B01J31/12 , C07B31/00 , C07B35/04 , C07B61/00 , C07C35/44 , C07C45/00 , C07C49/323 , C07C67/00 , C07J1/00 , C07J5/00 , C07J7/00 , C07J9/00 , B01J31/04 , B01J31/02
CPC分类号： C07J7/0055 , C07J1/0011 , C07J9/00
摘要： Derivatives of selenium as dehydrogenation agents employed in the presence of an oxidation agent consisting of oxidized derivatives of possibly substiuted iodoaromatic compounds, particularly where the derivatives of selenium are employed in catalytic amounts; as well as a process of dehydrogenation 3-oxygenated steroids into the corresponding 3-oxygenated .DELTA..sup.1,4 steroids.
摘要翻译：硒作为脱氢剂的衍生物用于存在由可能取代的碘代芳族化合物的氧化衍生物组成的氧化剂的存在下，特别是当硒的衍生物以催化量使用时; 以及将3-氧化类固醇脱氢成相应的3-氧化的DELTA 1,4类固醇的过程。

28. 发明授权

US4370497A Oxidation process using tellurium oxide catalysts 失效
标题翻译：使用碲氧化物催化剂的氧化工艺
公开(公告)号：US4370497A
公开(公告)日：1983-01-25
申请号：US175847
申请日：1980-08-07
申请人： Derek H. R. Barton , Steven V. Ley , Clive A. Meerholz
发明人： Derek H. R. Barton , Steven V. Ley , Clive A. Meerholz
IPC分类号： C07C46/06 , C07C50/02 , C07C273/18 , C07C275/28 , C07C321/28 , C07C329/18 , C07C395/00 , C07J9/00 , C07J31/00 , C07C127/19
CPC分类号： C07C395/00 , C07C273/1809 , C07C321/28 , C07C329/18 , C07C46/06 , C07C50/02 , C07J31/003 , C07J31/006 , C07J9/00
摘要： The present invention relates to the use of telluroxides as mild and selective oxidizing agents serving to oxidize certain functions, notably >C.dbd.S groups, in the presence of other relatively easily oxidized functions which remain unaffected; telluroxides of interest as oxidizing agents include, for example, compounds of the formula: ##STR1## wherein R and R.sup.1, which may be the same or different, each represent an optionally substituted aryl or heterocyclic group; or R and R.sup.1 together with the tellurium atom therebetween represent a heterocyclic ring, which may contain one or more further heteroatoms, and which may carry substituents and/or fused aromatic rings.
摘要翻译：本发明涉及在存在其它相对容易被氧化的功能而不受影响的情况下，用作氧化某些功能的特氟隆（特别是> C = S基）的氟氯化铁作为温和和选择性氧化剂的用途; 感兴趣的氧化铁作为氧化剂包括例如下式的化合物：其中R和R 1可以相同或不同，各自表示任选取代的芳基或杂环基; 或R和R 1与它们之间的碲原子表示杂环，其可以含有一个或多个另外的杂原子，并且其可以携带取代基和/或稠合芳环。

29. 发明授权

US4298676A Optical filter agents and photographic products and processes containing same 失效
标题翻译：光学过滤剂和含有它们的摄影产品和方法
公开(公告)号：US4298676A
公开(公告)日：1981-11-03
申请号：US89559
申请日：1979-10-29
申请人： Derek H. R. Barton , Irena Y. Bronstein-Bonte , Lloyd D. Taylor
发明人： Derek H. R. Barton , Irena Y. Bronstein-Bonte , Lloyd D. Taylor
IPC分类号： G03C8/48 , G03C1/40 , G03C1/10 , G03C1/84 , G03C5/54
CPC分类号： G03C8/48
摘要： Optical filter agents and photographic products and processes using same are disclosed. The optical filter agents are pH-sensitive hydrazone compounds conforming to the following structural formula: ##STR1## where R is any group which can provide a double bond for conjugation with the ##STR2## portion of the compound to provide light-absorbing capability or color for the agent at a pH above its pKa, X is a substituent of R providing at least one electron-withdrawing group and each R' can be defined as any substituent that does not impair the light-absorbing capacity of the compound at a pH above the pKa thereof. The pH-sensitive optical filter agents have a highly colored light-absorbing form at a pH above the pKa and are substantially non-absorbing at a pH below the pKa. The pH-sensitive optical filter agents are useful in photographic film units and processes for the protection of photoexposed photosensitive elements against the occurence of fogging during in-light development.
摘要翻译：公开了使用其的光学过滤剂和照相产品和方法。光学过滤剂是符合以下结构式的pH敏感腙化合物：其中R是可以提供双键与化合物的部分缀合以提供光吸收能力或颜色的任何基团对于高于其pKa的pH的试剂，X是提供至少一个吸电子基团的R的取代基，并且每个R'可以被定义为在上述pH以上不会损害化合物的光吸收能力的任何取代基其pKa。 pH敏感的光学过滤剂在高于pKa的pH下具有高度着色的光吸收形式，并且在低于pKa的pH下基本上不吸收。 pH敏感的光学滤光剂可用于照相胶片单元和用于保护光敏元件的过程，以防止在光照显影过程中发生起雾。

30. 发明授权

US4269925A Polymeric optical filter agents and photographic products and processes containing same 失效
标题翻译：聚合物光学滤光剂和含有它们的摄影产品和方法
公开(公告)号：US4269925A
公开(公告)日：1981-05-26
申请号：US089558
申请日：1979-10-29
申请人： Derek H. R. Barton , Irena Y. Bronstein-Bonte , Lloyd D. Taylor
发明人： Derek H. R. Barton , Irena Y. Bronstein-Bonte , Lloyd D. Taylor
IPC分类号： G03C8/48 , G03C1/40 , G03C1/10 , G03C1/84 , G03C5/54
CPC分类号： G03C8/48
摘要： Polymeric optical filter agents and photographic products and processes using same are disclosed. The polymeric optical filter agents are pH-sensitive optical filter agents comprising polymeric backbone units having the following hydrazone moiety: ##STR1## where R is a group which can provide a double bond for conjugation with the ##STR2## portion of the moiety to provide light-absorbing capability for the agent at a pH above its pKa, and X represents a substituent of R providing at least one electron-withdrawing group. The polymeric pH-sensitive optical filter agents have a highly colored light-absorbing form at a pH above the pKa and are substantially non-absorbing at a pH below the pKa. The polymeric optical filter agents are useful in photographic film units and processes for the protection of photoexposed photosensitive elements against the occurence of fogging during in-light development.
摘要翻译：公开了聚合物光学滤光剂和使用它们的照相产品和方法。聚合物光学过滤剂是pH敏感的光学过滤剂，其包含具有以下腙部分的聚合物主链单元：其中R是能够提供双键以与该部分的“IMAGE”部分缀合以提供光的基团 - 在高于其pKa的pH下的试剂的吸收能力，X表示提供至少一个吸电子基团的R的取代基。聚合物pH敏感光学过滤剂在高于pKa的pH下具有高度着色的光吸收形式，并且在低于pKa的pH下基本上不吸收。聚合物光学滤光剂可用于照相胶片单元和用于保护光敏元件免于在光照显影过程中发生起雾的过程。

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