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    • 7. 发明申请
    • MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES
    • 微波诱导的一些新型2-芳基醛及其类似物的单步合成
    • WO2010097811A4
    • 2010-11-04
    • PCT/IN2010000110
    • 2010-02-25
    • COUNCIL SCIENT IND RESSINHA ARUN KUMARSHARMA ABHISHEKKUMAR RAKESHSHARMA NAINA
    • SINHA ARUN KUMARSHARMA ABHISHEKKUMAR RAKESHSHARMA NAINA
    • C07C45/30C07C47/228C07C47/23C07C47/24C07C47/277C07C311/49C07D317/54
    • C07C45/28C07C45/30C07C249/16C07C311/49C07D317/54C07C47/228C07C47/24C07C47/23C07C47/277
    • 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 1min- 30min, 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.
    • 本发明提供了制备一些新的2-芳基和2,2-二芳基醛和类似物的方法,所述醛和类似物是用于商业上重要的非甾体抗炎药,包括萘普生,氟比洛芬和有效的抗癌候选药物包括苯抑制素通过 采用芳基烯烃形式的容易获得的底物以及溶剂形式的环境友好的水性反应条件,例如水和DMSO或二氧六环的混合物和试剂N-溴代琥珀酰亚胺,N-碘代琥珀酰亚胺,N-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,反应时间从1分钟至30分钟不等,取决于微波或常规加热,而不使用昂贵的过渡金属催化剂或路易斯酸/碱,产率从35-55变化 %,取决于所用的溶剂和基材。 所开发的方法提供了一种干净而方便的替代方案,以取代使用昂贵且危险的过渡金属催化剂和路易斯酸/碱的常规多步骤方案的各种医学上重要的基于2-芳基和2,2-二芳基醛的支架。
    • 9. 发明申请
    • ONE POT MULTICOMPONENT SYNTHESIS OF SOME NOVEL HYDROXY STILBENE DERIVATIVES WITH ALPHA, BETA-CARBONYL CONJUGATION UNDER MICROWAVE IRRADIATION
    • 一种具有ALPHA的新型羟基苯并苯衍生物的多糖合成,微波辐射下的碳纳米管结合
    • WO2010113005A2
    • 2010-10-07
    • PCT/IB2010000675
    • 2010-03-26
    • COUNCIL SCIENT IND RESSHARMA ABHISHEKSINHA ARUN KUMARKUMAR RAKESHSHARMA NAINA
    • SHARMA ABHISHEKSINHA ARUN KUMARKUMAR RAKESHSHARMA NAINA
    • C07C41/30
    • A61K36/482C07D317/54C07D333/16
    • The present invention provides a method for the preparation of some novel commercially important multiconjugated 2- or 4-hydroxy substituted stilbenes including lithospermic acid based stilbene analogues possessing an a, ß-unsaturated carboxylic acid moiety i.e. (C6-C2-C6-C3 chain) with wide ranging applications as potent pharmcophores for diverse ailments including diabetes and cardiovascular disorders, besides finding usage in non-linear optical devices and optoelectronics etc. The method provides a unique one pot multicomponent approach wherein 3-4 step reaction sequences viz. condensation, decarboxylation and Heck coupling occur simultaneously either the need for decarboxylating/protection-deprotection agents or individual isolation of highly reactive intermediates which results in an enhanced yield of desired products and reduced reaction times. The present invention dispenses with the hitherto indispensable requirement for multistep approaches for a diverse range of hydroxy stilbene derivatives through a one pot muticomponent synthetic strategy.
    • 本发明提供一种制备一些新的商业上重要的多结合的2-或4-羟基取代的二苯乙烯的方法,包括具有α,β-不饱和羧酸部分的(例如(C 6 -C 2 -C 6 -C 3链) 广泛的应用作为各种疾病(包括糖尿病和心血管疾病)的强大药剂,除了在非线性光学器件和光电子等中使用外,还提供了独特的一锅多组分方法,其中3-4步反应顺序即 缩合,脱羧和Heck偶联同时发生脱羧/保护脱保护剂的需要或高反应中间体的单独分离,这导致所需产物的产率提高和反应时间缩短。 本发明通过一锅多组分合成策略免除了对多种范围的羟基二苯乙烯衍生物的多步法的迄今不可或缺的要求。