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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

US5472957A Chemical compounds and process 失效
标题翻译：化合物和工艺
公开(公告)号：US5472957A
公开(公告)日：1995-12-05
申请号：US104496
申请日：1993-08-10
申请人： Robert H. Hesse , Ezio Rizzardo , Derek H. R. Barton
发明人： Robert H. Hesse , Ezio Rizzardo , Derek H. R. Barton
IPC分类号： A61K31/59
CPC分类号： A61K31/59
摘要： The invention provides novel compositions for use in pharmaceutical and veterinary medicine which contain 1.alpha.-hydroxy vitamin D compounds. Particular compositions are described which contain steroids which induce or assist in combatting osteoporosis together with 1.alpha.-hydroxy vitamin D.sub.3 or 1.alpha.,25-dihydroxy vitamin D.sub.3. Methods of treatment of diseases are also provided including many which are resistant to vitamin D.sub.3, in particular bone diseases.
摘要翻译：本发明提供了用于含有1α-羟基维生素D化合物的药物和兽医学中的新型组合物。描述了包含诱导或协助与1α-羟基维生素D3或1α，25-二羟基维生素D3一起对抗骨质疏松症的类固醇的特定组合物。还提供了治疗疾病的方法，包括许多对维生素D3，特别是骨疾病有抗性的疾病。

3. 发明授权

US4670190A 1-.alpha.-hydroxy vitamin D compounds and process for preparing same 失效
标题翻译： 1-羟基维生素D化合物及其制备方法
公开(公告)号：US4670190A
公开(公告)日：1987-06-02
申请号：US657270
申请日：1984-10-03
申请人： Robert H. Hesse , Ezzio Rizzardo , Derek H. R. Barton
发明人： Robert H. Hesse , Ezzio Rizzardo , Derek H. R. Barton
IPC分类号： C07J9/00
CPC分类号： C07J9/00
摘要： The invention provides novel 1.alpha.-hydroxy vitamin D compounds and a method for their preparation from 1.alpha.-hydroxy-25-hydrogen cholesta-5,7-dienes by irradiation and isomerization techniques. The invention also includes the said 1.alpha.-hydroxy-25-hydrogen-cholesta-5,7-dienes and the corresponding cholest-5-enes.The new compounds may be obtained in a crystalline form substantially free from isomeric or other impurities arising from manufacture.
摘要翻译：本发明提供新颖的1α-羟基维生素D化合物及其通过照射和异构化技术从1α-羟基-25-氢胆甾醇-5,7-二烯制备的方法。本发明还包括所述的1α-羟基-25-氢 - 胆甾烯-5,7-二烯和相应的胆甾-5-烯。新化合物可以以基本上不含由制造产生的异构体或其它杂质的结晶形式获得。

4. 发明授权

US4529437A Herbicides 失效
标题翻译：除草剂
公开(公告)号：US4529437A
公开(公告)日：1985-07-16
申请号：US159517
申请日：1980-06-16
申请人： Roberto Colle , Franco Gozzo , Ciro Preziuso , Antony G. M. Barrett , Derek H. R. Barton
发明人： Roberto Colle , Franco Gozzo , Ciro Preziuso , Antony G. M. Barrett , Derek H. R. Barton
IPC分类号： A01N47/42 , C07C335/28 , C07C335/30 , C07C335/32 , C07D295/215 , A01N43/40 , A01N43/84 , A01N47/30
CPC分类号： C07D295/215 , A01N47/42 , C07C335/28 , C07C335/30 , C07C335/32
摘要： Thiocarbamoyl-guanidine derivatives having herbicide activity are disclosed.The process for their preparation and their use as herbicides are disclosed too.
摘要翻译：公开了具有除草剂活性的硫代氨基甲酰基 - 胍衍生物。其制备方法及其作为除草剂的用途也被公开。

5. 发明授权

US4339593A Process for the manufacture of 3,6-dialkyl resorcylic acid esters 失效
标题翻译：制备3,6-二烷基间苯二甲酸酯的方法
公开(公告)号：US4339593A
公开(公告)日：1982-07-13
申请号：US216901
申请日：1980-12-16
申请人： Brian J. Willis , David I. Lerner , Derek H. R. Barton
发明人： Brian J. Willis , David I. Lerner , Derek H. R. Barton
IPC分类号： B01J27/00 , C07B61/00 , C07C67/317 , C07C69/88 , C11B9/00 , C07C69/76
CPC分类号： C07C67/317 , C07C69/88
摘要： Dialkyl-substituted .beta.-resorcylic acid esters having the structure: ##STR1## wherein each of R.sub.1, R.sub.2, and R.sub.3 is lower alkyl may be readily prepared by reacting the corresponding dihydroresorcylic acid esters with sulfuryl chloride. These compounds, particularly, methyl 3,6-dimethyl-resorcylate and methyl 3-ethyl-6-methyl-resorcylate, have oakmoss-like odors rendering them valuable as perfume ingredients.
摘要翻译：具有以下结构的二烷基取代的β-间苯二甲酸酯：其中R 1，R 2和R 3各自为低级烷基可以通过使相应的二氢间苯胂酸酯与磺酰氯反应而容易地制备。这些化合物，特别是3,6-二甲基 - 间苯二甲酸甲酯和3-乙基-6-甲基 - 间苯二甲酸甲酯，具有橡木般的气味，使得它们作为香料成分是有价值的。

6. 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。

7. 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。

8. 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。

9. 发明授权

US4234515A Preparation of N,N-difluoroamines 失效
标题翻译：制备N，N-二氟胺
公开(公告)号：US4234515A
公开(公告)日：1980-11-18
申请号：US904338
申请日：1978-05-09
申请人： Derek H. R. Barton , Robert H. Hesse
发明人： Derek H. R. Barton , Robert H. Hesse
IPC分类号： C07C291/00 , C07H9/04 , C07H13/06 , C07C85/18
CPC分类号： C07H9/04
摘要： N,N-difluoroamines are prepared by fluorination of compounds containing a >C.dbd.N-- bond using molecular fluorine or a hypofluorite in which the fluoroxy group is bonded to an inert electron attracting group, such hypofluorites including fluoroalkyl hypofluorites such as trifluoromethyl hypofluorite. The fluorination is advantageously conducted in the presence of an alkanol or other nucleophilic compound. Suitable starting materials include imino ethers and esters and aliphatic and aromatic Schiff's bases, use of the latter being particularly convenient.
摘要翻译：使用分子氟或氟氧基与惰性吸电子基团结合的次氟酸荧光氟化含有C = N-键的化合物制备N，N-二氟胺，这种次氟酸盐包括氟代烷基次氟酸酯如三氟甲基次氟酸荧光。氟化有利地在烷醇或其它亲核化合物的存在下进行。合适的起始原料包括亚氨基醚和酯以及脂族和芳香族席夫碱，后者的使用特别方便。

10. 发明授权

US4220588A Chemical processes 失效
标题翻译：化学工艺
公开(公告)号：US4220588A
公开(公告)日：1980-09-02
申请号：US8074
申请日：1979-01-31
申请人： Derek H. R. Barton , David J. Lester , Steven V. Ley
发明人： Derek H. R. Barton , David J. Lester , Steven V. Ley
IPC分类号： C07J9/00 , C07J51/00 , C07J71/00
CPC分类号： C07J51/00 , C07J71/0005 , C07J9/00
摘要： .alpha.,.beta.-Unsaturated aldehydes and ketones are prepared by reaction of an arylseleninic anhydride with an aldehyde or ketone having at least one hydrogen atom in the .alpha.-position which is or can be in the syn-configuration with respect to at least one hydrogen atom in the said .beta.-position. The ketones used as starting material especially include perhydrophenanthrene ketones such as steroid ketones and the arylseleninic anhydride used may for example be benzeneseleninic anhydride.
摘要翻译： α，β-不饱和醛和酮通过芳基硒
酸酐与具有至少一个氢原子的醛或酮在α-位上反应来制备，该位置相对于至少一个氢原子是或可以处于syn构型在所述beta版本中。用作起始原料的酮特别包括全氢菲酮如类固醇酮，所用的芳基硒茚酸可以是苯硒
酸酐。

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