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1. 发明授权

US6093812A Process for the stereospecific synthesis of azetidinones 失效
标题翻译：立体定向合成氮杂环丁酮的方法
公开(公告)号：US6093812A
公开(公告)日：2000-07-25
申请号：US179008
申请日：1994-01-07
申请人： Tiruvettipuram K. Thiruvengadam , Chou-Hong Tann , Junning Lee , Timothy McAllister , Cesar Colon , Derek H. R. Barton , Ronald Breslow , Anantha Sudhakar
发明人： Tiruvettipuram K. Thiruvengadam , Chou-Hong Tann , Junning Lee , Timothy McAllister , Cesar Colon , Derek H. R. Barton , Ronald Breslow , Anantha Sudhakar
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/695 , A61P3/06 , A61P9/10 , C07D205/08 , C07D205/085 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/10 , C07D409/04 , C07D413/10 , C07F7/08 , C07F7/10 , C07F7/18
CPC分类号： C07D401/04 , C07D205/08 , C07D205/085 , C07D403/04 , C07D405/04 , C07D405/10 , C07D409/04 , C07F7/0812 , C07F7/186 , C07F7/1892
摘要： This invention provides an improved process for producing azetidinones. More particularly, this invention provides the steps of producing an trans-azetidinone represented by the formula ##STR1## from a carboxylic acid R.sup.2 --D--CH.sub.2 COOH, an aldehyde R.sup.1 --A--CHO and an amine RNH.sub.2, by the steps of: (a1) converting a carboxylic acid to the corresponding acid chloride; (b1) deprotonating a chiral oxazolidinone and treating the resulting anion with the product of step (a1); (c1) enolizing the product of step (b1) and condensing with the aldehyde; (d1) hydrolyzing the product of step (c1); (e1) condensing the product of step (d1) with the amine; and (f1) cyclizing the product of step (e1). Alternatively, the process comprises (a2) enolizing the product of step (b1) and condensing, in the presence of a Lewis acid, with a Schiff's base prepared from the aldehyde and the amine; and (b2) cyclizing the product of step (a2).
摘要翻译：本发明提供了一种生产氮杂环丁酮的改进方法。更具体地，本发明提供了以下步骤：通过以下步骤，由羧酸R2-D-CH2COOH，醛R1-A-CHO和胺RNH2制备由式表示的反式氮杂环丁酮的步骤：（a1）羧酸与相应的酰氯反应; （b1）将手性恶唑烷酮去质子化并用步骤（a1）的产物处理所得的阴离子; （c1）使步骤（b1）的产物烯化并与醛缩合; （d1）水解步骤（c1）的产物; （e1）将步骤（d1）的产物与胺缩合; 和（f1）使步骤（e1）的产物环化。或者，该方法包括（a2）使路易斯酸存在下的步骤（b1）的产物烯醇化并与由醛和胺制备的席夫碱缩合; 和（b2）使步骤（a2）的产物环化。

2. 发明授权

US4471137A Highly sterically hindered guanidines and process for the production thereof 失效
标题翻译：高度位阻的胍及其制备方法
公开(公告)号：US4471137A
公开(公告)日：1984-09-11
申请号：US398219
申请日：1982-07-14
申请人： Derek H. R. Barton , John D. Elliott , Stephan D. Gero
发明人： Derek H. R. Barton , John D. Elliott , Stephan D. Gero
IPC分类号： C07C67/00 , C07C239/00 , C07C279/04 , C07C129/00 , C07C128/00
CPC分类号： C07C279/04
摘要： Compounds of the formula ##STR1## in which R.sub.1, R.sub.1 ', R.sub.2, R.sub.2 ' and R.sub.3 independently represent a C.sub.1-6 alkyl radical, in addition to which R.sub.3 may represent a hydrogen atom, the alkyl radicals together containing in all at least 8 carbon atoms, are provided for use as highly sterically hindered bases in chemical syntheses.
摘要翻译：其中R1，R1'，R2，R2'和R3独立地表示C1-6烷基的式“IMAGE”的化合物，除了R3可以表示氢原子之外，烷基一起含有至少8个碳原子被提供用作化学合成中的高空间位阻碱。

3. 发明授权

US4284558A Chemical process for fluorinating a tertiary carbon atom in the steroid nucleus 失效
标题翻译：用于氟化类固醇核中叔碳原子的化学方法
公开(公告)号：US4284558A
公开(公告)日：1981-08-18
申请号：US775879
申请日：1977-03-09
申请人： Derek H. R. Barton , Robert H. Hesse
发明人： Derek H. R. Barton , Robert H. Hesse
IPC分类号： C07B31/00 , C07B39/00 , C07C17/00 , C07C17/10 , C07C19/08 , C07C19/10 , C07C19/12 , C07C23/20 , C07C67/00 , C07J1/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J41/00 , C07J53/00 , C07J75/00
CPC分类号： C07J53/00 , C07B39/00 , C07C17/10 , C07J1/0011 , C07J1/0025 , C07J41/005 , C07J5/0076 , C07J7/002 , C07J7/0055 , C07J9/00
摘要： Saturated organic compounds containing a hydrogen atom bound to a tertiary carbon atom may be electrophilically fluorinated by reaction with an electrophilic fluorinating agent such as molecular fluorine or trifluoromethyl hypofluorite under conditions whereby the formation of free fluorine radicals is suppressed, e.g. by the presence of a free radical inhibitor such as oxygen or nitrobenzene, the reactants being substantially homogeneously dispersed in a liquid medium, e.g. a solvent medium such as fluorotrichloromethane or chloroform/fluorotrichloromethane, so that the said hydrogen atom is electrophilically replaced by a fluorine atom. The fluorination is highly selective and, in the case of complex substrates such as saturated steroids which contain a number of tertiary C--H bonds, may be substantially completely confined to replacement of the hydrogen atom at the tertiary carbon atom which has the highest electron density about the C--H bond. The electron density and thus the direction of the fluorination may be controlled by appropriate selection of substituent groupings in the substrate molecule.Novel 14.alpha.-fluorosteroids are also disclosed, including compounds having valuable androgenic or progestational activity and useful synthetic intermediates.
摘要翻译：含有与叔碳原子结合的氢原子的饱和有机化合物可以通过与亲电氟化剂如分子氟或三氟甲基次氟酸荧光反应，在抑制游离氟自由基形成的条件下进行亲电氟化。通过存在自由基抑制剂如氧或硝基苯，反应物基本均匀地分散在液体介质中，例如，溶剂介质如氟三氯甲烷或氯仿/氟三氯甲烷，使所述氢原子被氟原子亲电取代。氟化是高度选择性的，并且在复杂的底物例如含有多个叔CH键的饱和类固醇的情况下，可以基本上完全限制于在具有最高电子密度的叔碳原子上的氢原子的取代 CH键。可以通过适当选择底物分子中的取代基组来控制电子密度以及氟化方向。还公开了新的14种α-氟甾类，包括具有有价值的雄激素或促孕活性的化合物和有用的合成中间体。

4. 发明授权

US4174318A Alkylative cleavage of azetidinone disulfides 失效
标题翻译：氮杂环丁烷二硫化物的烷基化裂解
公开(公告)号：US4174318A
公开(公告)日：1979-11-13
申请号：US726425
申请日：1976-09-22
申请人： Derek H. R. Barton , Peter G. Sammes , Graham Hewitt , Brian E. Looker , William G. E. Underwood
发明人： Derek H. R. Barton , Peter G. Sammes , Graham Hewitt , Brian E. Looker , William G. E. Underwood
IPC分类号： C07D205/095 , C07D499/00 , C07D205/08
CPC分类号： C07D499/00 , C07D205/095
摘要： Novel semisynthetic 4-thio-azetidin-2-one derivatives of use in the production of cephalosporins, penicillins and related .beta.-lactam antibiotic compounds are provided by cleavage reactions involving the corresponding 4-dithio-azetidin-2-one derivative or a suitable thiazoline derivative, which starting materials may be obtained from penicillins without changing the configuration of the .beta.-lactam structure desired in the final product.
摘要翻译：用于生产头孢菌素，青霉素和相关β-内酰胺抗生素化合物的新型半合成4-硫代 - 氮杂环丁烷-2-酮衍生物通过涉及相应的4-二硫代氮杂环丁-2-酮衍生物或合适的噻唑啉衍生物，其起始材料可以从青霉素获得，而不改变最终产物中所需的β-内酰胺结构的构型。

5. 发明授权

US4159326A Hydrogenation process for the preparation of 5,6 cis- and 5,6-trans-10,19-dihydro-vitamin D compounds using transistion metal catalysts 失效
标题翻译：使用交联金属催化剂制备5,6顺式和5,6-反-10,19-二氢维生素D化合物的氢化方法
公开(公告)号：US4159326A
公开(公告)日：1979-06-26
申请号：US801825
申请日：1977-05-31
申请人： Derek H. R. Barton , Robert H. Hesse
发明人： Derek H. R. Barton , Robert H. Hesse
IPC分类号： A61K31/59 , A61P3/02 , B01J31/00 , C07C67/00 , C07C401/00
CPC分类号： C07C401/00 , C07C2101/14 , C07C2102/24
摘要： A process for the preparation of 5,6-cis- and 5,6-trans-10,19-dihydro-vitamin D derivatives which comprises hydrogenating a corresponding vitamin D compound in the presence of a ligand-coordinated homogeneous transition metal catalyst whereby the C-19 methylene group of the vitamin D compound is converted into a methyl group.
摘要翻译：一种制备5,6-顺式和5,6-反式-10,19-二氢 - 维生素D衍生物的方法，包括在配位体配位的均相过渡金属催化剂存在下氢化相应的维生素D化合物，由此将维生素D化合物的C-19亚甲基转化为甲基。

6. 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。

7. 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。

8. 发明授权

US5756852A Co-oxidation of H.sub.2 S and saturated hydrocarbons 失效
标题翻译： H2S和饱和烃的共同氧化
公开(公告)号：US5756852A
公开(公告)日：1998-05-26
申请号：US730206
申请日：1996-10-15
申请人： Derek H. R. Barton
发明人： Derek H. R. Barton
IPC分类号： B01J31/20 , C01B17/04 , C01B17/05 , C07B61/00 , C07C45/28 , C07C45/33 , C07C49/403
CPC分类号： C07C45/33 , C01B17/05 , C07C45/28
摘要： Process for the catalytic oxidation of a saturated hydrocarbon to obtain a ketone which involves carrying out the oxidation simultaneously with the oxidation of H.sub.2 S to form elemental sulfur and the ketone.
摘要翻译：用于饱和烃的催化氧化的方法，以获得酮，其涉及在与硫化物的氧化的同时进行氧化以形成元素硫和酮。

9. 发明授权

US4689410A Novel 23-dihydro-oxazolyl steroids 失效
标题翻译：新型23-二氢 - 恶唑基类固醇
公开(公告)号：US4689410A
公开(公告)日：1987-08-25
申请号：US787657
申请日：1985-10-16
申请人： Derek H. R. Barton , Samir Z. Zard , Jocelyne Wozniak
发明人： Derek H. R. Barton , Samir Z. Zard , Jocelyne Wozniak
IPC分类号： C07J7/00 , C07J43/00 , C07J17/00
CPC分类号： C07J43/003 , C07J7/002
摘要： Novel 23-dihydro-oxazolyl steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the A, B, C and D rings may contain 1 to 3 double bonds and may be optionally substituted with one or more members of the group consisting of --OH, protected hydroxyl, .dbd.0, protected keto, halogen alkyl or alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms and the dotted line indicates the optional presence of a second bond useful for the preparation of 20-keto-pregnanes and novel intermediates.
摘要翻译：式（Ⅰ）的新型2,3-二氢 - 恶唑基类固醇，其中R 1选自氢和甲基，R 2选自甲基和乙基，R 3和R 4分别选自氢和1至4个碳原子的烷基，A，B，C和D环可以含有1至3个双键，并且可以任选地被一个或多个由-OH，被保护的羟基，保护的酮基，卤素烷基或1至4个碳原子的烷氧基和2至4个碳原子的链烯基和炔基，虚线表示任选存在可用于制备20-酮 - 孕烷和新中间体的第二键。

10. 发明授权

US4501701A 20-Isocyano-.DELTA..sup.17(20) -steroids 失效
标题翻译： 20-Isocyano-DELTA 17（20） - 类
公开(公告)号：US4501701A
公开(公告)日：1985-02-26
申请号：US281552
申请日：1981-07-07
申请人： Derek H. R. Barton , William B. Motherwell , Sammir Z. Zard
发明人： Derek H. R. Barton , William B. Motherwell , Sammir Z. Zard
IPC分类号： C07J75/00 , C07F9/40 , C07J7/00 , C07J41/00 , C07J1/00
CPC分类号： C07J41/005 , C07F9/4006
摘要： Novel 20-isocyano-.DELTA..sup.17(20) -steroids of the formula ##STR1## wherein R.sup.1 is selected from the group consisting of (1) hydrogen, (2) alkyl of 1 to 4 carbon atoms optionally substituted with a member of the group consisting of halogen, an oxygen function and a nitrogen function and (3) alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms, Alk.sub.1, is alkyl of 1 to 8 carbon atoms and the A,B,C, and D rings may contain one or more double bonds and may be optionally substituted with at least one member of the group consisting of --OH, .dbd.0, halogens, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms and a process for their preparation and their use to prepare 17.alpha.-ol-20-keto steroids.
摘要翻译：新颖的20-异氰基-TATA 17（20） - 式Ⅰ的化合物，其中R 1选自（1）氢，（2）1至4个碳原子的烷基，任选被由卤素，氧官能团和氮官能团组成的组，（3）2至4个碳原子的烯基和炔基，R2是1至4个碳原子的烷基，Alk1是1至8个碳原子的烷基，A， B，C和D环可以含有一个或多个双键，并且可以任选地被至少一个由-OH，= O，卤素，1-4个碳原子的烷基和烷氧基组成的组中的一个取代，以及烯基和炔基 2至4个碳原子的化合物及其制备方法及其用于制备17α-20-O-酮类固醇的方法。

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