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21. 发明授权

US5233086A Intermediates for the preparation of an antiviral agent 失效
标题翻译：用于制备抗病毒剂的中间体
公开(公告)号：US5233086A
公开(公告)日：1993-08-03
申请号：US961946
申请日：1992-10-16
申请人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
发明人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
IPC分类号： C07B57/00 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/68 , C07C69/743 , C07C309/73 , C07D473/00
CPC分类号： C07D473/00 , C07B57/00 , C07C309/73 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/68 , C07C69/743 , C07C2101/04
摘要： Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylene-cyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
摘要翻译：外消旋Feist酸用（R） - （+） - α-甲基苄胺处理，得到（1R-反式）-3-亚甲基 - 环丙烷-1,2-二羧酸，（R）-α-甲基苄胺（1:1）盐。然后将该盐转化为（1R-反式）-3-亚甲基-1,2-环丙烷二羧酸二甲酯，其是制备抗病毒剂[1R-（1α，2β，3α） ] -2-氨基-9- [2,3-双（羟甲基）环丁基] -1,9-二氢-6H-嘌呤-6-酮。改进的方法还可以从分辨率中回收外消旋的Feist酸。

22. 发明授权

US4973747A Process for preparing 3-hydroxy 2-keto acids 失效
标题翻译：制备3-羟基2-酮酸的方法
公开(公告)号：US4973747A
公开(公告)日：1990-11-27
申请号：US394369
申请日：1989-08-15
申请人： Janak Singh , Richard H. Mueller
发明人： Janak Singh , Richard H. Mueller
IPC分类号： C07C51/373 , C07C51/31 , C07C59/215 , C07C59/90 , C07D303/48
CPC分类号： C07D303/48 , C07C51/31
摘要： A process has now been discovered by which an intermediate in preparation of antibiotics ##STR1## may be directly derived from the substrate ##STR2## by treatment with aqueous solutions of MHCO.sub.3 and MOH, wherein: R.sup.1, R.sup.2 and R.sup.3 are each independently alkyl, alkenyl, alkynyl, substituted alkyl, substituted alkenyl, substituted alkynyl, aryl, or substituted aryl;M is alkali metal (such as Na, Li, or K); andX is halogen.

23. 发明申请

US20110201795A1 Methods of Producing C-Aryl Glucoside SGLT2 Inhibitors 审中-公开
标题翻译：生产C-Aryl Glucoside SGLT2抑制剂的方法
公开(公告)号：US20110201795A1
公开(公告)日：2011-08-18
申请号：US13093430
申请日：2011-04-25
申请人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
发明人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
IPC分类号： C07H1/00 , C07H23/00 , C07H15/02
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

24. 发明授权

US07486430B2 Single-crystal-silicon 3D micromirror 失效
标题翻译：单晶硅3D微镜
公开(公告)号：US07486430B2
公开(公告)日：2009-02-03
申请号：US11345891
申请日：2006-02-02
申请人： Chih Kiong Terence Gan , Ajay Agarwal , Janak Singh , Xiaolin Zhang
发明人： Chih Kiong Terence Gan , Ajay Agarwal , Janak Singh , Xiaolin Zhang
IPC分类号： G02B26/00 , G02B26/08
CPC分类号： G02B26/0866
摘要： In a 3D free space micromirror device, a mirror plate is joined with actuators through flexible springs where the other ends of the actuators have fixed support on the substrate. Single crystal silicon and aluminum are used as bi-morph materials with silicon dioxide providing electrical isolation between the two. Thickness variation in the microstructure is achieved by two-step p-n junction formed in a p-type substrate. Thick and thin n-silicon layer formation and DRIE cut mechanisms are employed in such a way that all the thick and thin silicon components of the structure are released simultaneously avoiding overetch which can be detrimental to the thin flexural springs. Working prototypes of the device have been found suitable for any optical switching array architecture where deflections up to 10 degrees are required.
摘要翻译：在3D自由空间微镜装置中，镜板通过柔性弹簧与致动器连接，致动器的另一端在基板上具有固定的支撑。单晶硅和铝被用作双变体材料，二氧化硅在两者之间提供电隔离。通过在p型衬底中形成的两步p-n结实现微结构的厚度变化。使用厚且薄的n型硅层形成和DRIE切割机构，使得结构的所有厚和薄的硅部件同时释放，避免了可能对薄弯曲弹簧有害的过蚀刻。已经发现器件的工作原型适用于需要高达10度偏转的任何光学开关阵列架构。

25. 发明授权

US06858459B2 Method of fabricating micro-mirror switching device 失效
标题翻译：制造微镜开关装置的方法
公开(公告)号：US06858459B2
公开(公告)日：2005-02-22
申请号：US10154279
申请日：2002-05-23
申请人： Janak Singh , Uppili Sridhar , Ranganathan Nagarajan , Quanbo Zou
发明人： Janak Singh , Uppili Sridhar , Ranganathan Nagarajan , Quanbo Zou
IPC分类号： H01L21/00 , H01L31/0232
CPC分类号： B81C1/00142 , B81B2201/042 , G02B26/0841
摘要： Method of fabricating a micro-mirror switching device in single crystal silicon are described. The device is fabricated as three main elements: silicon mirror plate with metal-mirror, secondary actuator, and hinge/spring mechanism to integrate the mirror plate with the actuator. p-n junction is first formed on p-type silicon. Trenches are then etched in n-silicon to define the device element boundaries and filled with silicon dioxide. Three layers of sacrificial oxide and two structural poly-silicon layers are deposited and patterned to form device elements. Novel release processes, consisting of backside electrochemical etching in potassium-hydroxide, reactive ion etching to expose oxide-filled trenches from the bottom, and hydrofluoric acid etching of sacrificial oxide layers and oxide in silicon trenches, form the silicon blocks; those that are not attached to structural poly-silicon are sacrificed and those that are attached are left in place to hold together the switching device elements.
摘要翻译：描述了在单晶硅中制造微镜开关器件的方法。该装置被制造为三个主要元件：具有金属镜的硅镜板，二次致动器和用于将镜面板与致动器集成的铰链/弹簧机构。 p-n结首先在p型硅上形成。然后在n硅中蚀刻沟槽以限定器件元件边界并填充二氧化硅。沉积和图案化三层牺牲氧化物和两个结构多晶硅层以形成器件元件。由氢氧化钾中的背面电化学蚀刻，从底部暴露氧化物填充的沟槽的反应离子蚀刻和硅沟槽中的牺牲氧化物层和氧化物的氢氟酸蚀刻组成的新型释放过程形成硅块; 牺牲未附着于结构多晶硅的那些，并且将附着的那些留在适当位置以将开关元件元件保持在一起。

26. 发明授权

US5618946A 7-oxabicycloheptane carboxylic acid prostaglandin analog intermediates useful in the preparation of anti-thrombotic and anti-vasospastic compounds and method for preparing same 失效
标题翻译：可用于制备抗血栓形成和抗血管痉挛性化合物的7-氧杂双环庚烷羧酸前列腺素类似物中间体及其制备方法
公开(公告)号：US5618946A
公开(公告)日：1997-04-08
申请号：US609153
申请日：1996-02-29
申请人： Michael A. Poss , Paul D. Pansegrau , Shaopeng Wang , John K. Thottathil , Janak Singh , Richard H. Mueller
发明人： Michael A. Poss , Paul D. Pansegrau , Shaopeng Wang , John K. Thottathil , Janak Singh , Richard H. Mueller
IPC分类号： C07D491/18 , C07D493/08 , C07D493/18 , C07D491/02 , C07D407/14
CPC分类号： C07D493/08
摘要： The present invention relates to novel 7-oxabicycloheptane carboxylic acid prostaglandin analog intermediates which may be used to prepare a final anti-thrombotic, anti-vasospastic product, and to methods for preparing the same.
摘要翻译：本发明涉及可用于制备最终抗血栓形成，抗血管扩张产物的新型7-氧杂双环庚烷羧酸前列腺素类似物中间体及其制备方法。

27. 发明授权

US5525726A Process for the preparation of an antiviral agent 失效
标题翻译：制备抗病毒剂的方法
公开(公告)号：US5525726A
公开(公告)日：1996-06-11
申请号：US150308
申请日：1993-11-12
申请人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
发明人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
IPC分类号： C07B57/00 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/743 , C07C309/73 , C07D473/00 , A61K31/52 , C07D473/18
CPC分类号： C07D473/00 , C07B57/00 , C07C309/73 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/743 , C07C2101/04
摘要： Racemic Feist's acid is treated with (R)-(+) -.alpha.-methylbenzylamine to yield (1R-trans)-3-methylene -cyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzyl-amine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
摘要翻译：外消旋Feist酸用（R） - （+） - α-甲基苄胺处理，得到（1R-反式）-3-亚甲基 - 环丙烷-1,2-二羧酸，（R）-α-甲基苄基胺（1： 1）盐。然后将该盐转化为（1R-反式）-3-亚甲基-1,2-环丙烷二羧酸二甲酯，其是制备抗病毒剂[1R-（1α，2β，3α） ] -2-氨基-9- [2,3-双（羟甲基）环丁基] -1,9-二氢-6H-嘌呤-6-酮。改进的方法还可以从分辨率中回收外消旋的Feist酸。

28. 发明授权

US5412134A Process for preparing diprotected 2,3-hydroxymethyl cyclobutanol 失效
标题翻译：制备双保护的2,3-羟甲基环丁醇的方法
公开(公告)号：US5412134A
公开(公告)日：1995-05-02
申请号：US888077
申请日：1992-05-26
申请人： Janak Singh , Gregory S. Bisacchi , Richard H. Mueller
发明人： Janak Singh , Gregory S. Bisacchi , Richard H. Mueller
IPC分类号： C07C69/78 , C07C29/143 , C07C35/04 , C07C43/164 , C07C51/347 , C07C59/29 , C07C67/28 , C07C67/29 , C07F7/18 , C07D473/18
CPC分类号： C07F7/1892 , C07C67/29
摘要： The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, diphenylsilane in the presence of tris(triphenylphosphine) rhodium (I) chloride, or iridium tetrachloride to yield the corresponding diprotected cyclobutanol. This compound is useful as an intermediate in the preparation of antiviral agents.
摘要翻译：在三（三苯基膦）氯化铑（I）或四氯化铱存在下，用二烷基铝氯化物，烷基二氯化铝，三烷基铝化合物，二苯基硅烷处理式“IMAGE”的保护的环丁酮，得到相应的二保护的环丁醇。该化合物可用作制备抗病毒剂的中间体。

29. 发明授权

US5281716A Method for preparing 7-oxabicycloheptyl substituted oxazole amide prostaglandin analog intermediates useful in the preparation of anti-thrombotic and anti-vasospastic compounds 失效
标题翻译：制备7-氧杂二环庚基取代的恶唑酰胺前列腺素类似物中间体的方法，用于制备抗血栓形成和抗血管痉挛性化合物
公开(公告)号：US5281716A
公开(公告)日：1994-01-25
申请号：US20948
申请日：1993-02-22
申请人： Richard H. Mueller , Janak Singh
发明人： Richard H. Mueller , Janak Singh
IPC分类号： A61K31/42 , A61P7/02 , A61P9/00 , C07D493/08
CPC分类号： C07D493/08
摘要： A method is provided for preparing oxazole intermediates of the structure ##STR1## (wherein R is alkyl) wherein an oxazoline of the structure ##STR2## is oxidized employing an oxidizing agent such as cupric bromide, a base such as 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), and a non-hydride donor amine base such as hexamethylenetetraamine (HMTA). The resulting oxazole may be hydrolyzed to the final anti-thrombotic - anti-vasospastic compounds.
摘要翻译：提供了一种制备结构式（其中R是烷基）的恶唑中间体的方法，其中使用氧化剂如溴化铜将结构式“恶唑啉”氧化，碱如1,8-二氮杂双环[ 5.4.0]十一碳-7-烯（DBU）和非氢化物供体胺碱如六亚甲基四胺（HMTA）。所得恶唑可以水解成最终的抗血栓形成 - 抗血管痉挛性化合物。

30. 发明授权

US5237096A Process for the preparation of an antiviral agent 失效
公开(公告)号：US5237096A
公开(公告)日：1993-08-17
申请号：US961806
申请日：1992-10-16
申请人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
发明人： Jollie D. Godfrey, Jr. , Richard H. Mueller , Thomas P. Kissick , Janak Singh
IPC分类号： C07B57/00 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/68 , C07C69/743 , C07C309/73 , C07D473/00
CPC分类号： C07D473/00 , C07B57/00 , C07C309/73 , C07C45/58 , C07C49/753 , C07C51/487 , C07C61/35 , C07C69/68 , C07C69/743 , C07C2101/04
摘要： Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.

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