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1. 发明授权

US5055604A Process for preparing prostaglandin analogs using organozirconium compounds 失效
标题翻译：使用有机化合物制备PROSTAGLANDIN模拟物的方法
公开(公告)号：US5055604A
公开(公告)日：1991-10-08
申请号：US510349
申请日：1990-04-17
申请人： Kevin A. Babiak , James R. Behling , John H. Dygos , John S. Ng
发明人： Kevin A. Babiak , James R. Behling , John H. Dygos , John S. Ng
IPC分类号： B01J31/02 , C07B61/00 , C07C405/00 , C07F1/08 , C07F7/18
CPC分类号： C07F1/08 , C07C405/00
摘要： A process for preparing a prostaglandin derivative by reacting an alkyne with zirconocene chloride hydride to produce a zirconium intermediate which is reacted with an alkyllithium and a first copper reagent selected from R.sup.2 Cu(CN)Li or the mixture CuCN and R.sup.2 Li to produce a higher order cuprate complex intermediate and reacting the higher order cuprate complex intermediate with a cyclopentenone to produce the prostaglandin derivative.

2. 发明授权

US5252763A Process for preparing prostaglandin analogs 失效
标题翻译：前列腺素类似物的制备方法
公开(公告)号：US5252763A
公开(公告)日：1993-10-12
申请号：US911334
申请日：1992-07-08
申请人： Kevin A. Babiak , James R. Behling , John H. Dygos , John S. Ng
发明人： Kevin A. Babiak , James R. Behling , John H. Dygos , John S. Ng
IPC分类号： C07C405/00 , C07F1/08 , C07F7/18 , C07C61/20
CPC分类号： C07C405/00 , C07F1/08
摘要： A process for preparing higher order cuprate complexes by reacting an alkyne with zirconocene chloride hydride to produce a zirconium intermediate which is reacted with an alkyllithium and a first copper reagent selected from R.sup.2 Cu(CN)Li or the mixture CuCN and R.sup.2 Li to produce a higher order cuprate complex.
摘要翻译：通过使炔与二茂锆氯化氢反应制备锆中间体与烷基锂和选自R2Cu（CN）Li或CuCN和R2Li混合物的第一铜试剂反应以产生更高级的锆中间体的方法铜酸盐复合物

3. 发明授权

US5106750A Enantio- and regioselective synthesis of organic compounds using enol esters as irreversible transacylation reagents 失效
标题翻译：有机化合物的有机合成和有机合成作为不可逆的交联试剂
公开(公告)号：US5106750A
公开(公告)日：1992-04-21
申请号：US396723
申请日：1989-08-24
申请人： Chi-Huey Wong , Yi-Fong Wang , William J. Hennen , Kevin A. Babiak , John H. Dygos , John S. Ng
发明人： Chi-Huey Wong , Yi-Fong Wang , William J. Hennen , Kevin A. Babiak , John H. Dygos , John S. Ng
IPC分类号： C12P7/62 , C12P9/00 , C12P13/00 , C12P17/02 , C12P19/02 , C12P19/44 , C12P41/00
CPC分类号： C12P41/004 , C12P17/02 , C12P19/02 , C12P19/44 , C12P7/62 , C12P9/00
摘要： A process for irreversible regio- and stereoselective enzyme catalyzed acylation of alcohols using enol esters as acylating reagents is disclosed. The present invention permits the selective modification of hydroxyl group(s) of chiral and meso alcohols, including sugars, organometallics, and glycosides. The enol freed upon transesterification rapidly tautomerizes to the corresponding volatile aldehyde or ketone thereby preventing the reverse reaction from occurring.

4. 发明授权

US4910310A Synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives 失效
标题翻译： N-取代的1,5-二脱氧-1,5-亚氨基-L-岩藻糖醇衍生物的合成
公开(公告)号：US4910310A
公开(公告)日：1990-03-20
申请号：US252846
申请日：1988-10-03
申请人： Arthur L. Campbell , James R. Behling , Kevin A. Babiak , John S. Ng , Richard A. Mueller , George W. J. Fleet
发明人： Arthur L. Campbell , James R. Behling , Kevin A. Babiak , John S. Ng , Richard A. Mueller , George W. J. Fleet
IPC分类号： C07D307/62 , C07C211/46 , C07D211/46 , C07D491/04 , C07D491/056 , C07D493/04 , C07H9/04
CPC分类号： C07D491/04 , C07D211/46
摘要： Novel intermediates and method for the chemical synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives are provided. A preferred intermediate is 1,5-dideoxy-1,5-imino-3, 4-O-isopropylidene-L-fucitol which is used to prepare the HIV inhibitor 1,5-dideoxy-1,5-imino-[N-.omega.-methyl caproate]-L-fucitol. These compounds are prepared in a short synthesis from the known compound 2,3-O-isopropylidene-D-lyxono-1,4-lactone or in a multi-step synthesis from D-galactose.

5. 发明授权

US5011958A Process for preparing higher order cuprate complexes 失效
标题翻译：制备高级铜酸盐络合物的方法
公开(公告)号：US5011958A
公开(公告)日：1991-04-30
申请号：US427067
申请日：1989-10-25
申请人： Arthur L. Campbell , James R. Behling , John S. Ng , Kevin A. Babiak
发明人： Arthur L. Campbell , James R. Behling , John S. Ng , Kevin A. Babiak
IPC分类号： C07F1/08 , C07F7/22
CPC分类号： C07F1/08 , C07F7/2212
摘要： This invention encompasses a process for preparing higher order cuprate complexes which contain a carbanion for the formation of carbon to carbon bonds in reactions such as epoxide addition. The complex is formed by reacting a first cuprate complex with a stannane such that the carbanion to be used to form carbon to carbon bonds is transferred from the stannane to the first cuprate complex to form a different higher order cuprate complex. This process permits the in situ preparation of a higher order cuprate complex having the carbanion desired to be used in a synthetic reaction. Higher order cuprate complexes derived from the reaction of a cuprate complex with 1,2-bis-tri-n-butylstannyl ethylene are particularly useful for the addition to epoxides to form vinyl tin intermediates useful for preparing omega side chains of prostaglandins.
摘要翻译：本发明包括一种制备高级铜酸盐配合物的方法，其中含有用于在诸如环氧化物添加的反应中形成碳 - 碳键的碳负离子。络合物通过使第一铜酸盐络合物与锡烷反应形成，使得用于形成碳 - 碳键的碳负离子从锡烷转移到第一铜酸盐络合物以形成不同的高级铜酸盐络合物。该方法允许原位制备具有期望在合成反应中使用的碳负离子的高级铜酸盐络合物。衍生自铜酸盐络合物与1,2-双 - 三正丁基甲锡烷基乙烯反应的高级铜酸盐络合物特别可用于加入环氧化物以形成可用于制备前列腺素的ω侧链的乙烯基锡中间体。

6. 发明授权

US5104990A Process for the preparation of 3-aryl-3-aminoalkyl-2,6-dioxohexahydropyridines 失效
标题翻译：制备3-芳基-3-氨基甲酰基-2,6-二氧代甲基吡啶的方法
公开(公告)号：US5104990A
公开(公告)日：1992-04-14
申请号：US486027
申请日：1990-02-27
申请人： John H. Dygos , Kathleen T. McLaughlin , John S. Ng , Kalidas Paul
发明人： John H. Dygos , Kathleen T. McLaughlin , John S. Ng , Kalidas Paul
IPC分类号： C07D211/88 , C07D401/04
CPC分类号： C07D211/88
摘要： Disclosed is a process for the preparation of 3-aryl-3-aminoalkyl-2,6-dioxohexahydropridines and particularly the compounds 3-[3-(dimethylamino)propyl]-3-(3-methoxyphenyl)-4, 4-dimethyl-2,6-piperidinedione, monohydrochloride, which is useful as an antidepressant.the process of the present invention comprises the condensation of a sterically hindered nitrile with a sterically hindered .alpha., .beta.-unsaturated diester to produce a nitrile diester. These compounds can then undergo acid catalyzed cyclization and decarboalkoxylation in a one step process to provide the desired 3-aryl-3-aminoalkyl-2,6-dioxohexahydropyridine.

7. 发明授权

US5220019A Process for the preparation of diethyl 2-]2-cyano-5-(dimethylamino)-2-(3-methoxyphenyl)-1,1-dimethylpentyl]prop andioate 失效
标题翻译：制备2-] 2-氰基-5-（二甲基氨基）-2-（3-甲氧基苯基）-1,1-二甲基戊基]丙二酸二乙酯的方法
公开(公告)号：US5220019A
公开(公告)日：1993-06-15
申请号：US859189
申请日：1992-03-27
申请人： John H. Dygos , Kathleen T. McLaughlin , John S. Ng , Kalidas Paul
发明人： John H. Dygos , Kathleen T. McLaughlin , John S. Ng , Kalidas Paul
IPC分类号： C07D211/88
CPC分类号： C07D211/88
摘要： Disclosed is a process for the preparation of 3-aryl-3-aminoalkyl-2,6-dioxohexahydropridines and particularly the compound 3-[3-(dimethylamino)propyl]3-(3 methoxyphenyl)-4, 4-dimethyl-2,6-piperidinedione, monohydrochloride, which is useful as an antidepressant.The process of the present invention comprises the condensation of a sterically hindered nitrile with a sterically hindered .alpha.,.beta.-unsaturated diester to produce a nitrile diester. These compounds can then undergo acid catalyzed cyclization and decarboalkoxylation in a one step process to provide the desired 3-aryl-3-aminoalkyl-2,6 -dioxohexahydropyridine.
摘要翻译：公开了制备3-芳基-3-氨基烷基-2,6-二氧代六氢吡啶的方法，特别是化合物3- [3-（二甲基氨基）丙基] -3-（3-甲氧基苯基）-4,4-二甲基-2- 6-哌啶二酮，一盐酸盐，其可用作抗抑郁药。本发明的方法包括将空间位阻腈与空间位阻的α，β-不饱和二酯缩合以制备腈二酯。然后这些化合物可以在一步法中进行酸催化环化和脱羰基烷氧基化，得到所需的3-芳基-3-氨基烷基-2,6-二氧代六氢吡啶。

8. 发明授权

US6127556A Epoxide formation by continuous in-situ synthesis process 失效
标题翻译：通过连续原位合成过程形成环氧化物
公开(公告)号：US6127556A
公开(公告)日：2000-10-03
申请号：US991598
申请日：1997-12-16
申请人： Chin Liu , John S. Ng , James R. Behling , Arthur L. Campbell
发明人： Chin Liu , John S. Ng , James R. Behling , Arthur L. Campbell
IPC分类号： C07D301/00 , C07C213/04 , C07C215/28 , C07D301/02 , C07D301/30 , C07D303/36 , C07D317/62
CPC分类号： C07D317/62 , C07D303/36
摘要： In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80.degree. C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0.degree. C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.
摘要翻译：在制备其中被保护的氨基醛与卤代甲基有机金属试剂在合适的溶剂中在-80℃以上反应的方法中，其中所述卤代甲基有机金属试剂是由有机金属试剂和二卤代甲烷之间的反应形成的，改进包括将保护的氨基醛流入保持在低于0℃的混合区，同时使所述混合区中的卤代甲基有机金属试剂流动，以使所述混合区与所述受保护的氨基醛接触，并且还从所述混合区抽出反应产物所述保护的氨基醛和所述卤代甲基有机金属试剂。

9. 发明授权

US07189864B2 Method of preparing intermediates useful in synthesis of retroviral protease inhibitors 失效
标题翻译：制备可用于合成逆转录病毒蛋白酶抑制剂的中间体的方法
公开(公告)号：US07189864B2
公开(公告)日：2007-03-13
申请号：US10962746
申请日：2004-10-13
申请人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman
发明人： John S. Ng , Claire A. Przybyla , Richard A. Mueller , Michael L. Vazquez , Daniel P. Getman
IPC分类号： C07C221/00 , C07D301/02
CPC分类号： C07K5/06191 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C04B35/632 , C07B2200/07 , C07C213/00 , C07C213/02 , C07C213/08 , C07C269/06 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D303/36 , C07D307/85 , C07D401/12 , C07K5/0207 , C07K5/021 , C07K5/06026 , C07K5/06139 , C07C215/08 , C07C215/28 , C07C271/16
摘要： A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.
摘要翻译：对于易于大规模制备基于羟基脲的手性HIV蛋白酶抑制剂的中间体描述了合成。该方法包括由手性α氨基醛形成非对映选择性环氧化物。

10. 发明授权

US06335441B1 5&bgr;-cyano-substituted steroid compounds 失效
标题翻译： 5β-氰基取代的类固醇化合物
公开(公告)号：US06335441B1
公开(公告)日：2002-01-01
申请号：US09583158
申请日：2000-05-30
申请人： John S. Ng , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
发明人： John S. Ng , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
IPC分类号： C07J5300
CPC分类号： C07J71/00 , C07J21/00 , C07J21/003 , C07J31/006 , C07J53/00 , C07J53/002 , C07J71/0015 , C12P33/005 , C12P33/10 , C12Q1/02
摘要： Novel 5&bgr;-cyano steroid compounds including compounds of Formula VII: wherein A—A, B—B, R3, R8 and R9 are as defined in the specification.
摘要翻译：包括式VII化合物的新型5β-氰基类固醇化合物：其中A-A，B-B，R 3，R 8和R 9如说明书中所定义。

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