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1. 发明授权

US4981995A Method for producing ibuprofen 失效
标题翻译：生产布洛芬的方法
公开(公告)号：US4981995A
公开(公告)日：1991-01-01
申请号：US500645
申请日：1990-03-28
申请人： Varadaraj Elango , Mark A. Murphy , Brad L. Smith , Kenneth G. Davenport , Graham N. Mott , Edward G. Zey , Gary L. Moss
发明人： Varadaraj Elango , Mark A. Murphy , Brad L. Smith , Kenneth G. Davenport , Graham N. Mott , Edward G. Zey , Gary L. Moss
IPC分类号： B01J31/24 , C07C45/46 , C07C51/12 , C07C57/30
CPC分类号： B01J31/2404 , B01J31/24 , C07C45/46 , C07C51/12 , B01J2231/34 , B01J2531/824 , Y02P20/584
摘要： A method is provided for the preparation of ibuprofen by carbonylating 1-(4'-isobutylphenyl)ethanol (IBPE) with carbon monoxide in an acidic aqueous medium, e.g. containing at least 10% of water based on the weight of IBPE initially added, at a temperature of at least about 10.degree. C. and a carbon monoxide pressure of at least about 500 psig, and in the presence of (1) a catalyst complex consisting essentially of a palladium compound in which the palladium has a valence of zero to 2 and is complexed with at least one monodentate phosphine ligand miscible with the organic phase of the reaction medium, the phosphorus/palladium mole ratio in said palladium compound and ligand being at least about 2:1 when the palladium/IBPE mole ratio is such that palladium=1 and IBPE=10,000 or more; (2) dissociated hydrogen ions from an acid which is substantially completely ionizable in dilute aqueous solution such that the mole ratio of hydrogen ions to IBPE added to the reaction zone is at least about 0.15; and, (3) dissociated halide ions such that the mole ratio of halide ions to IBPE added to the reaction zone is at least about 0.15. Advantageously, a hydrogen halide is the source of hydrogen ions and halide ions. The carbonylation is preferably integrated with a method of producing IBPE from isobutylbenzene wherein the latter compound is subjected to Friedel-Crafts reaction with an acetylating agent to produce 4-isobutylacetophenone, which is then reduced with hydrogen in the presence of a hydrogenation catalyst, or with a reducing agent containing available hydrogen, to obtain IBPE. The palladium catalyst complex can be precipitated from an organic phase of the carbonylation reaction which typically includes the ibuprofen product. The precipitated catalyst complex can be recycled without further treatment.
摘要翻译：提供了一种通过在酸性水性介质中将1-（4'-异丁基苯基）乙醇（IBPE）与一氧化碳羰基化来制备布洛芬的方法，例如，在至少约10℃的温度和至少约500psig的一氧化碳压力下，在（1）催化剂络合物的存在下，基于最初加入的IBPE的重量，含有至少10％的水基本上由钯化合物组成，其中钯的价数为0至2，并且与至少一种与反应介质的有机相可混溶的单齿膦配体络合，所述钯化合物和配体中的磷/钯摩尔比为当钯/ IBPE摩尔比使得钯= 1和IBPE = 10,000或更高时，至少约2:1; （2）从在稀水溶液中基本完全可离子化的酸离解氢离子使得加入到反应区中的氢离子与IBPE的摩尔比至少为约0.15; 和（3）离解的卤离子使得加入反应区的卤离子与IBPE的摩尔比至少为约0.15。有利地，卤化氢是氢离子和卤离子的来源。羰基化优选与从异丁基苯生产IBPE的方法相结合，其中后一种化合物与乙酰化剂进行Friedel-Crafts反应以产生4-异丁基苯乙酮，然后在氢化催化剂存在下用氢还原，或与含有可用氢的还原剂，以获得IBPE。钯催化剂络合物可以从通常包括布洛芬产物的羰基化反应的有机相中沉淀出来。沉淀的催化剂络合物可以循环使用，无需进一步处理。

2. 发明授权

US4908476A Synthesis of 2-(4-hydroxyphenoxy)alkanoic acids 失效
标题翻译： 2-（4-羟基苯氧基）链烷酸的合成
公开(公告)号：US4908476A
公开(公告)日：1990-03-13
申请号：US170728
申请日：1988-03-21
申请人： Varadaraj Elango , Kenneth G. Davenport
发明人： Varadaraj Elango , Kenneth G. Davenport
IPC分类号： C07C51/00 , C07C51/09 , C07C51/367 , C07C59/125 , C07C59/64 , C07C67/00
CPC分类号： C07C51/09 , C07C51/367
摘要： A method for synthesizing 2-(4-hydroxyphenoxy)alkanoic acids by reacting a hydroxyaromatic ketone derivative with a 2-substituted alkanoic acid under basic conditions and thereafter oxidizing the intermediate with subsequent hydrolysis.

3. 发明授权

US5008439A Synthesis of 2-(4-hydroxyphenoxy) alkanoic acid esters 失效
标题翻译： 2-（4-羟基苯氧基）烷酸酯的合成
公开(公告)号：US5008439A
公开(公告)日：1991-04-16
申请号：US170711
申请日：1988-03-21
申请人： Varadaraj Elango , Kenneth G. Davenport
发明人： Varadaraj Elango , Kenneth G. Davenport
IPC分类号： C07C67/31 , C07C69/712 , C07C69/736
CPC分类号： C07C67/31 , C07C69/712
摘要： A method for synthesizing 2-(4-hydroxyphenoxy)alkanoic acid esters by reacting a hydroxyaromatic ketone derivative with a 2-substituted alkanoic acid ester under basic conditions and thereafter oxidizing the intermediate with subsequent hydrolysis.

4. 发明授权

US5405987A Process for preparing pyridine and quinoline derivatives 失效
标题翻译：制备吡啶和喹啉衍生物的方法
公开(公告)号：US5405987A
公开(公告)日：1995-04-11
申请号：US676683
申请日：1991-03-28
申请人： Varadaraj Elango , Donald R. Larkin , John R. Fritch , Michael P. Bodman , Werner H. Mueller , Bernard F. Gupton , John C. Saukaitis
发明人： Varadaraj Elango , Donald R. Larkin , John R. Fritch , Michael P. Bodman , Werner H. Mueller , Bernard F. Gupton , John C. Saukaitis
IPC分类号： C07C239/08 , C07C239/18 , C07D213/79 , C07D213/80 , C07D215/48 , C07D215/54 , C07D401/04 , C07C255/00 , C07C229/24
CPC分类号： C07D213/79 , C07C239/18 , C07D213/80 , C07D215/54 , C07D401/04
摘要： The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives which can be dehydrated to 2-aminobut-2-ene dioic acid derivatives, which can be subsequently converted to pyridine and quinoline derivatives.
摘要翻译：本发明涉及可以脱水成2-氨基丁-2-烯二酸衍生物的取代和未取代的N-羟基-2-氨基丁二酸二酸衍生物的方法，其可随后转化为吡啶和喹啉衍生物。

5. 发明授权

US5235090A Synthesis of 2-(4'-aminophenyloxy) alkanoic acids & acids & esters & their derivatives 失效
标题翻译： 2-（4'-氨基苯氧基）链烷酸及其酯及其衍生物的合成
公开(公告)号：US5235090A
公开(公告)日：1993-08-10
申请号：US979399
申请日：1992-11-19
申请人： Varadaraj Elango
发明人： Varadaraj Elango
IPC分类号： C07C217/84 , C07C231/10 , C07C233/25
CPC分类号： C07C231/10 , C07C217/84 , C07C233/25
摘要： A method for synthesizing 2-(4-amidophenoxy)alkanoic acids and esters and 2-(4-aminophenoxy)alkanoic acids and esters by reacting a hydroxyaromatic ketone derivative with a 2-substituted alkanoic acid or ester under basic conditions and thereafter reacting with a hydroxylamine derivative and conducting a Beckmann Rearrangement with subsequent solvolysis.
摘要翻译：通过在碱性条件下使羟基芳族酮衍生物与2-取代的链烷酸或酯反应，然后与一种（4-氨基苯氧基）链烷酸和酯反应而合成2-（4-氨基苯氧基）羟胺衍生物，并进行Beckmann重排，随后溶剂解。

6. 依法登记的发明

USH1760H Process for glycol esters of an alkali metal salt of 5-sulfoisophthalic acid 失效
标题翻译： 5-磺基间苯二甲酸碱金属盐的二醇酯的方法
公开(公告)号：USH1760H
公开(公告)日：1998-11-03
申请号：US780474
申请日：1997-01-08
申请人： Varadaraj Elango , William R. Lee , Jeffrey S. Hurley , Cheryl A. Littau
发明人： Varadaraj Elango , William R. Lee , Jeffrey S. Hurley , Cheryl A. Littau
IPC分类号： C07C303/06 , C07C303/22 , C07C309/32 , C07C309/58 , C07C311/00
CPC分类号： C07C303/32 , C07C303/06 , C07C303/22 , C07C309/58
摘要： A process for preparing bis alkylene glycol esters of an alkali metal salt of 5-sulfoisophthalic acid. The subject compound is useful in preparing modified polyesters which can be dyed with basic or cationic dyes. The process is economical and low cost since intermediate reaction products are not purified.
摘要翻译：一种制备5-磺基间苯二甲酸的碱金属盐的双亚烷基二醇酯的方法。本发明化合物可用于制备可用碱性或阳离子染料染色的改性聚酯。由于中间反应产物不被纯化，所以该方法是经济且成本低的。

7. 发明授权

US5225603A Preparation of 4-(6'-methoxy-2'-naphthyl)-3-buten-2-one 失效
标题翻译：制备4-（6'-甲氧基-2'-萘基）-3-丁烯-2-酮
公开(公告)号：US5225603A
公开(公告)日：1993-07-06
申请号：US211106
申请日：1988-06-17
申请人： Mohammad Aslam , Varadaraj Elango
发明人： Mohammad Aslam , Varadaraj Elango
IPC分类号： C07C45/62 , C07C45/68 , C07C49/255
CPC分类号： C07C49/255 , C07C45/62 , C07C45/68
摘要： An intermediate for the manufacture of nabumetone, 4-(6'-methoxy-2'-naphthyl)-3-buten-2-one, is prepared by contacting 2-bromo-6-methoxynaphphalene with methyl vinyl ketone in the presence of a palladium catalyst at from about 50.degree. C. to about 200.degree. C. for a time sufficient to cause substantially complete reaction to occur.
摘要翻译：通过使2-溴-6-甲氧基萘酚与甲基乙烯基酮在甲苯乙烯酮存在下接触来制备萘啶酮4-（6'-甲氧基-2'-萘基）-3-丁烯-2-酮的中间体钯催化剂在约50℃至约200℃下反应足以引起基本上完全反应的时间。

8. 发明授权

US06555704B1 Process for the carbonylation of arylalkyl halides 失效
标题翻译：芳基烷基卤羰基化的方法
公开(公告)号：US06555704B1
公开(公告)日：2003-04-29
申请号：US08445593
申请日：1995-05-22
申请人： Varadaraj Elango
发明人： Varadaraj Elango
IPC分类号： C07C5112
CPC分类号： C07C51/10 , C07C57/30
摘要： A method is provided for the preparation of alpha-aryl-propionic acids such as ibuprofen by carbonylating the corresponding 1-arylethyl halide in an acidic aqueous medium containing a palladium catalyst. In the preparation of ibuprofen, 1-(4′-isobutylphenyl)ethyl halide is reacted with carbon monoxide in an acidic aqueous medium containing a palladium catalyst.
摘要翻译：提供了一种通过在含有钯催化剂的酸性含水介质中羰基化相应的1-芳基乙基卤来制备α-芳基丙酸如布洛芬的方法。在布洛芬的制备中，1-（4'-异丁基苯基）乙基卤与含有钯催化剂的酸性水性介质中的一氧化碳反应。

9. 发明授权

US5322948A Process for preparing pyridinecarboxylic acid derivatives 失效
标题翻译：制备吡啶羧酸衍生物的方法
公开(公告)号：US5322948A
公开(公告)日：1994-06-21
申请号：US818396
申请日：1992-01-02
申请人： Varadaraj Elango , Donald R. Larkin , John R. Fritch , Michael P. Bodman , Werner H. Mueller , Bernard F. Gupton , John C. Saukaitis
发明人： Varadaraj Elango , Donald R. Larkin , John R. Fritch , Michael P. Bodman , Werner H. Mueller , Bernard F. Gupton , John C. Saukaitis
IPC分类号： C07C239/18 , C07C253/30 , C07C255/64 , C07D213/79 , C07D213/80 , C07D401/04 , C07D213/69
CPC分类号： C07D213/79 , C07C239/18 , C07C253/30 , C07C255/64 , C07D213/80 , C07D401/04
摘要： The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives. The invention also pertains to the use of N-hydroxy-2-aminoethane derivatives (including the N-hydroxy-2-aminobutane diacid derivatives) in the preparation of pyridine derivatives.
摘要翻译：本发明涉及制备取代和未取代的N-羟基-2-氨基丁烷二酸衍生物的方法。本发明还涉及N-羟基-2-氨基乙烷衍生物（包括N-羟基-2-氨基丁烷二酸衍生物）在制备吡啶衍生物中的用途。

10. 发明授权

US5012007A Method for producing 1-indanone derivatives 失效
标题翻译： 1-茚满酮衍生物的制备方法
公开(公告)号：US5012007A
公开(公告)日：1991-04-30
申请号：US417376
申请日：1989-10-05
申请人： Varadaraj Elango
发明人： Varadaraj Elango
IPC分类号： B01J27/12 , C07B61/00 , C07C33/20 , C07C45/46 , C07C45/49 , C07C45/71 , C07C49/67 , C07C49/747 , C07C221/00 , C07C225/30 , C07C319/20 , C07C323/22
CPC分类号： C07C49/67 , C07C33/20 , C07C45/46 , C07C45/49 , C07C45/71
摘要： A method is provided for the production of 2,2-diorgano-1-indanones, e.g., 2,2-dimethyl-1-indanone, by reacting an alcohol which is the corresponding (diorganosubstitutedmethyl)phenyl(or substitutedphenyl)carbinol, e.g., 2-methyl-1-phenyl-1-propanol, with carbon monoxide in the presence of a Lewis acid catalyst, e.g., hydrogen fluoride, with any substituents on the phenyl group of the alcohol being hydroxy or organo. The foregoing reaction is preferably integrated with the preparation of the feed alcohol by reducing the corresponding (diorganosubstitutedmethyl)phenyl(or substitutedphenyl)ketone, e.g., isobutyrophenone, with a reducing agent containing available hydrogen, e.g., sodium borohydride, or with hydrogen gas in the presence of a hydrogenation catalyst.

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