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    Microwave induced single step green synthesis of some novel 2-aryl aldehydes and their analogues
    3.
    发明授权
    Microwave induced single step green synthesis of some novel 2-aryl aldehydes and their analogues 失效
    微波诱导单步绿色合成一些新型2-芳基醛及其类似物

    公开(公告)号：US08779200B2

    公开(公告)日：2014-07-15

    申请号：US13203100

    申请日：2010-02-25

    申请人： Arun Kumar Sinha ,  Abhishek Sharma ,  Rakesh Kumar ,  Naina Sharma

    发明人： Arun Kumar Sinha ,  Abhishek Sharma ,  Rakesh Kumar ,  Naina Sharma

    IPC分类号： C07C241/00 ,  C07C47/00

    CPC分类号： C07C45/28 ,  C07C45/30 ,  C07C249/16 ,  C07C311/49 ,  C07D317/54 ,  C07C47/228 ,  C07C47/24 ,  C07C47/23 ,  C07C47/277

    摘要： The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N-iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1 min-30 min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55%, depending upon the solvent and substrate used. The developed method provides a clean and convenient alternative to access a diverse range of medicinally important 2-aryl and 2,2-diaryl aldehyde based scaffolds in lieu of the conventional multistep protocols employing expensive and hazardous transition metal catalysts and lewis acids/bases.

    摘要翻译： 本发明提供了一种制备一些新的2-芳基和2,2-二芳基醛和类似物的方法，其是用于商业上重要的非甾族抗炎药物的特权中间体，包括萘普生，氟比洛芬和有效的抗癌药物候选物，包括通过 使用易于获得的芳基烯烃底物的独特的单步合成方法以及溶剂形式的环境友好的水性反应条件，例如水和DMSO或二恶烷的混合物以及试剂N-溴琥珀酰亚胺，N-碘代琥珀酰亚胺，N-氯代氯代琥珀酰亚胺 和相转移催化剂如十六烷基三甲基溴化铵，N-己基氯化铵，反应时间为1分钟-30分钟，取决于微波或常规加热，不使用昂贵的过渡金属催化剂或路易斯酸/碱，产率从35 -55％，这取决于所用的溶剂和底物。 开发的方法提供了一种干净和方便的替代方案，以便获得各种各样的药物重要的2-芳基和2,2-二芳基醛基支架，代替常规的多步骤方案，其采用昂贵且危险的过渡金属催化剂和路易斯酸/碱。

    MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES
    4.
    发明申请
    MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES 失效
    微波诱导的单步绿色合成一些新型二芳基醛及其类似物

    公开(公告)号：US20120041234A1

    公开(公告)日：2012-02-16

    申请号：US13203100

    申请日：2010-02-25

    申请人： Arun Kumar Sinha ,  Abhishek Sharma ,  Rakesh Kumar ,  Naina Sharma

    发明人： Arun Kumar Sinha ,  Abhishek Sharma ,  Rakesh Kumar ,  Naina Sharma

    IPC分类号： C07C251/80 ,  C07C45/00 ,  B01J19/12 ,  C07C47/27

    CPC分类号： C07C45/28 ,  C07C45/30 ,  C07C249/16 ,  C07C311/49 ,  C07D317/54 ,  C07C47/228 ,  C07C47/24 ,  C07C47/23 ,  C07C47/277

    摘要： The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N-iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1 min-30 min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55%, depending upon the solvent and substrate used. The developed method provides a clean and convenient alternative to access a diverse range of medicinally important 2-aryl and 2,2-diaryl aldehyde based scaffolds in lieu of the conventional multistep protocols employing expensive and hazardous transition metal catalysts and lewis acids/bases.

    摘要翻译： 本发明提供了一种制备一些新的2-芳基和2,2-二芳基醛和类似物的方法，其是用于商业上重要的非甾族抗炎药物的特权中间体，包括萘普生，氟比洛芬和有效的抗癌药物候选物，包括通过 使用易于获得的芳基烯烃底物的独特的单步合成方法以及溶剂形式的环境友好的水性反应条件，例如水和DMSO或二恶烷的混合物以及试剂N-溴琥珀酰亚胺，N-碘代琥珀酰亚胺，N-氯代氯代琥珀酰亚胺 和相转移催化剂如十六烷基三甲基溴化铵，N-己基氯化铵，反应时间为1分钟-30分钟，取决于微波或常规加热，不使用昂贵的过渡金属催化剂或路易斯酸/碱，产率从35 -55％，这取决于所用的溶剂和底物。 开发的方法提供了一种干净和方便的替代方案，以便获得各种各样的药物重要的2-芳基和2,2-二芳基醛基支架，代替常规的多步骤方案，其采用昂贵且危险的过渡金属催化剂和路易斯酸/碱。

    Microwave induced one pot process for the preparation of arylethenes
    6.
    发明授权
    Microwave induced one pot process for the preparation of arylethenes 失效
    微波诱导一锅法制备芳纶

    公开(公告)号：US07759527B2

    公开(公告)日：2010-07-20

    申请号：US11691896

    申请日：2007-03-27

    申请人： Arun Kumar Sinha ,  Anuj A Sharma ,  Vinod Kumar

    发明人： Arun Kumar Sinha ,  Anuj A Sharma ,  Vinod Kumar

    IPC分类号： C07C41/01 ,  C07C37/00 ,  C07C67/00

    CPC分类号： C07C41/18 ,  C07C37/0555 ,  C07C37/50 ,  C07C37/82 ,  C07C41/26 ,  C07C43/23 ,  C07C39/20 ,  C07C43/215

    摘要： The invention entitled “A Microwave Induced One Pot Process for The Preparation of Arylethenes” provides a method for the preparation of commercially important 2- or 4-hydroxy substituted arylethenes like styrenes or stilbenes in one pot utilizing cheaper substrates in the form of 2- or 4-hydroxy substituted cinnamic acids and their derivatives as well as reagents in the form of base such as sodium hydroxide, potassium hydroxide, lithium hydroxide, sodium bicarbonate, sodium carbonate, potassium bicarbonate, potassium carbonate, ammonium acetate, imidazole, methylimidazole and the combination thereof, with or without solvent such as dimethylformamide, dimethylsulfoxide, ethylene glycol, diethylene glycol, acetonitrile, acetone, methyl imidazoles, ionic liquid, water and the like. The reaction time vary from 1 min-12 hrs and yield of the products from 49-76% depending upon the base, acid, substrate source of heating monomode or multimode microwave or conventional. It is important to mention that the presence of 2- or 4-hydroxy substitution at phenyl ring of cinnamic acids and their derivatives is essential requirements towards formation of corresponding arylethenes in one step.

    摘要翻译： 题为“A Microwave Induced One Pot Process for the Preparation of Arylehenes”的发明提供了一种在一个罐中制备商业上重要的2-或4-羟基取代的芳香醚如苯乙烯或二苯乙烯的方法，其使用2-或 4-羟基取代的肉桂酸及其衍生物以及碱的形式的试剂如氢氧化钠，氢氧化钾，氢氧化锂，碳酸氢钠，碳酸钠，碳酸氢钾，碳酸钾，乙酸铵，咪唑，甲基咪唑及其组合 有或没有溶剂如二甲基甲酰胺，二甲基亚砜，乙二醇，二甘醇，乙腈，丙酮，甲基咪唑，离子液体，水等。 反应时间从1分钟-12小时变化，产物的产率从49-76％变化，这取决于加热单模或多模微波或常规的碱，酸，底物来源。 重要的是提到在肉桂酸及其衍生物的苯环上存在2-或4-羟基取代是在一个步骤中形成相应的芳酰基的必要条件。

    Process for the preparation of substituted trans-cinnamaldehyde, a natural yellow dye, from phenylpropane derivatives
    7.
    发明授权
    Process for the preparation of substituted trans-cinnamaldehyde, a natural yellow dye, from phenylpropane derivatives 失效
    由苯基丙烷衍生物制备取代的反式肉桂醛（天然黄色染料）的方法

    公开(公告)号：US06566557B2

    公开(公告)日：2003-05-20

    申请号：US09805832

    申请日：2001-03-14

    申请人： Arun Kumar Sinha ,  Bhupendra Prasad Joshi ,  Ruchi Dogra

    发明人： Arun Kumar Sinha ,  Bhupendra Prasad Joshi ,  Ruchi Dogra

    IPC分类号： C07C4528

    CPC分类号： C09B61/00 ,  C07C45/28 ,  C07C45/30 ,  C07C47/277 ,  C09B57/00 ,  C07C47/54

    摘要： The present invention relates to the preparation of substituted trans-cinnamaldehyde, a natural yellow dye from Phenylpropane derivatives having R2—R3—R4—R5—R6 substitution, wherein R2 to R6 equal or different, being hydrogen or hydroxy or acyl or halogen or alkyl or heterocyclic or aryl or dioxymethylene or alkoxy groups, etc., by oxidizing the said phenylpropane derivatives using a oxidising agent such as 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) or p-chloranil or pyridinium chlorochromate (PCC) or tBuOOH or CrO3 with a catalytic amount of inorganic/organic acid or alumina, celite, and silica gel as a solid support for microwave irradiation and thus substituted trans-cinnamaldehydes, a natural yellow dye, are obtained in high yield ranging from 68-82%.

    摘要翻译： 本发明涉及取代的反式肉桂醛的制备，其是具有R2-R3-R4-R5-R6取代基的苯基丙烷衍生物的天然黄色染料，其中R2至R6相同或不同，为氢或羟基或酰基或卤素或烷基 或杂环或芳基或二氧亚甲基或烷氧基等，通过使用氧化剂如2,3-二氯-5,6-二氰基-1,4-苯醌（DDQ）或对氯醌来氧化所述苯基丙烷衍生物或 使用催化量的无机/有机酸或氧化铝，硅藻土和硅胶的氯铬酸吡啶鎓（PCC）或tBuOOH或CrO 3作为微波照射的固体支持物，从而以高产率获得取代的反式肉桂醛（天然黄色染料） 从68-82％。

    Single step green process for the preparation of substituted cinnamic esters with trans-selectivity
    8.
    发明授权
    Single step green process for the preparation of substituted cinnamic esters with trans-selectivity 失效
    用于制备具有反式选择性的取代肉桂酸酯的单步绿色方法

    公开(公告)号：US07741508B2

    公开(公告)日：2010-06-22

    申请号：US11728721

    申请日：2007-03-26

    申请人： Arun Kumar Sinha ,  Anuj Sharma ,  Anand Swaroop ,  Vinod Kumar

    发明人： Arun Kumar Sinha ,  Anuj Sharma ,  Anand Swaroop ,  Vinod Kumar

    IPC分类号： C07C69/76

    CPC分类号： C07C67/39 ,  C07C67/40 ,  C07C67/56 ,  Y02P20/582 ,  C07C69/734 ,  C07C69/618

    摘要： The invention provides a green process for direct oxidation of a large number of substituted or unsubstituted cinnamaldehydes or cinnamyl alcohols into the corresponding alkyl or aryl cinnamates in one step. The process of the present invention is a convenient and efficient green process for the preparation of various aryl or alkyl cinnamates under conventional, microwave and ultrasound directly from cinnamaldehydes or cinnamyl alcohols in the presence of an oxidizing agent, catalyst and an alcohol, with or without an organic solvent. These esters are immensely important compounds in flavor, perfumery and pharmaceutical industries. There are several prior arts available for the preparation of cinnamic esters, but all of them suffer from deficiencies such as use of expensive reagents and catalysts, harsh reaction conditions, use of toxic chemicals and others. In contrast, the present methodology is extremely simple and involves reaction of the substrate with an oxidizing agent mixed with a homogeneous or heterogeneous catalyst and an alcohol with or without organic solvent by stirring at room temperature or refluxing or under microwave or ultrasound irradiation to get the requisite products.

    摘要翻译： 本发明提供了在一个步骤中将大量取代或未取代的肉桂醛或肉桂醇直接氧化成相应的烷基或芳基肉桂酸酯的绿色方法。 本发明的方法是在常规的微波和超声波下直接从肉桂醛或肉桂醇在氧化剂，催化剂和醇存在下制备各种芳基或烷基肉桂酸酯的方法和有效的绿色方法，具有或不具有 有机溶剂。 这些酯是风味，香料和制药行业中非常重要的化合物。 有几种现有技术可用于制备肉桂酯，但是它们都存在诸如使用昂贵的试剂和催化剂，苛刻的反应条件，使用有毒化学品等缺点。 相比之下，本方法非常简单，包括在室温或回流下或在微波或超声波照射下，通过在室温或回流下或在微波或超声波照射下搅拌，使底物与均匀或多相催化剂和醇混合的氧化剂反应，得到 必备产品。

    Microwave induced process for the preparation of substituted 4-vinylphenols
    9.
    发明授权
    Microwave induced process for the preparation of substituted 4-vinylphenols 失效
    用于制备取代的4-乙烯基苯酚的微波诱导方法

    公开(公告)号：US06989467B2

    公开(公告)日：2006-01-24

    申请号：US10383253

    申请日：2003-03-07

    申请人： Arun Kumar Sinha ,  Bhupendra Prasad Joshi ,  Anuj Sharma

    发明人： Arun Kumar Sinha ,  Bhupendra Prasad Joshi ,  Anuj Sharma

    IPC分类号： C07C39/06

    CPC分类号： C07C43/23 ,  C07C37/20 ,  C07C41/30 ,  C07C51/353 ,  C07C51/38 ,  C07C59/52 ,  C07C59/64 ,  C07C39/20

    摘要： The present invention relates to “a microwave induced process for the preparation of 4-vinylphenols or its derivatives” in which commercially important FEMA GRAS approved perfumery and flavouring vinylphenols (i.e. hydroxystyrenes) namely 4-vinylguaiacol (FEMA GRAS No. 2675) and 4-vinylphenol (FEMA GRAS No. 3739) as well as other useful vinylphenols such as 2,6-dimethoxy-4-vinylphenol, 2-hydroxy-4-vinylphenol, 3-hydroxy-4-vinylphenol etc. by condensation of malonic acid and 4-hydroxyphenylaldehydes or its derivatives.

    摘要翻译： 本发明涉及“微波诱导的4-乙烯基苯酚或其衍生物的制备方法”，其中商业上重要的FEMA GRAS批准了香料和调味乙烯基苯酚（即羟基苯乙烯），即4-乙烯基愈创木酚（FEMA GRAS No.2675）和4- 乙烯基苯酚（FEMA GRAS No.3739）以及其它有用的乙烯基苯酚如2,6-二甲氧基-4-乙烯基苯酚，2-羟基-4-乙烯基苯酚，3-羟基-4-乙烯基苯酚等，通过丙二酸和4 - 羟基苯基醛或其衍生物。