4670-10-4Relevant academic research and scientific papers
Identification of N,N-arylalkyl-picolinamide derivatives targeting the RNA-binding protein HuR, by combining biophysical fragment-screening and molecular hybridization
Della Volpe,Linciano,Listro,Tumminelli,Amadio,Bonomo,Elgaher,Adam,Hirsch,Boeckler,Vasile,Rossi,Collina
, (2021/09/06)
Hu proteins are members of the RNA-binding protein (RBP) family and play a pivotal role in the regulation of post-transcriptional processes. Through interaction with selected mRNAs, RBPs regulate their function and stability; as a consequence, RBP dysregu
Desulfonylative Electrocarboxylation with Carbon Dioxide
Zhong, Jun-Song,Yang, Zi-Xin,Ding, Cheng-Lin,Huang, Ya-Feng,Zhao, Yi,Yan, Hong,Ye, Ke-Yin
supporting information, p. 16162 - 16170 (2021/09/02)
Electrocarboxylation of organic halides is one of the most investigated electrochemical approaches for converting thermodynamically inert carbon dioxide (CO2) into value-added carboxylic acids. By converting organic halides into their sulfone derivatives, we have developed a highly efficient electrochemical desulfonylative carboxylation protocol. Such a strategy takes advantage of CO2as the abundant C1 building block for the facile preparation of multifunctionalized carboxylic acids, including the nonsteroidal anti-inflammatory drug ibuprofen, under mild reaction conditions.
Stereoselective Total Synthesis of (-)-(2 S,4 R)-3′-Methoxyl Citreochlorol: Preparation and Use of New Proline-Based Auxiliary for Asymmetric Acetate Aldol Reaction
Sunnapu, Ranganayakulu,Banoth, Saikumar Naik,Reyno,Thomas, Aleena,Venugopal, Navyasree,Rajendar, Goreti
, p. 4103 - 4113 (2020/03/05)
The first stereoselective total synthesis of (-)-(2S,4R)-3′-methoxy citreochlorol and (-)-(2S,4S)-3′-methoxy citreochlorol is demonstrated. A proline-based imidazolidinone was synthesized and used as chiral auxiliary for asymmetric acetate aldol reaction to generate initial chirality in the targeted molecule. Geminal dichloromethane functionality was introduced by the addition of in situ generated dichloromethyllithium to Weinreb's amide functional group.
Convenient syntheses of 3-aryl-3,4-dihydroisocoumarins
Limaye, Rohan A.,Joseph, Augustine R.,Natu, Arun D.,Paradkar, Madhusudan V.
, p. 191 - 194 (2015/06/02)
A convenient method for the synthesis of naturally occurring 3,4-dihydroisocoumarins by judicious use of Friedel-Craft acylation, regioselective formylation and oxidative cyclisation reactions is described. O-methylated analogues of montroumarin and thunb
Simple access to 5-carboalkoxy-2,3-dihydro-4H-pyran-4-ones via domino acylative electrocyclization: The first three step total synthesis of the dihydronaphthopyran-4-one class of natural products
Ilangovan, Andivelu,Sakthivel, Palaniappan
, p. 55150 - 55161 (2015/01/16)
Intermolecular domino C-acylation/6π-oxaelectrocyclization between β-ketoesters and α,β-unsaturated acid chlorides took place readily in the presence of CaCl2 to afford a variety of polysubstituted 5-carboalkoxy-2,3-dihydro-4H-pyran-4-ones, in good yields. The products were successfully exploited as precursors, for a simple and efficient construction of a naphthalene fused pyran-4-one ring system. This intramolecular Friedel-Crafts acylative aromatization approach was useful for the synthesis of the phytogrowth inhibiting dihydronaphthopyranone class of natural products.
Controlled-deactivation cannabinergic ligands
Sharma, Rishi,Nikas, Spyros P.,Paronis, Carol A.,Wood, Jodianne T.,Halikhedkar, Aneetha,Guo, Jason Jianxin,Thakur, Ganesh A.,Kulkarni, Shashank,Benchama, Othman,Raghav, Jimit Girish,Gifford, Roger S.,J?rbe, Torbj?rn U. C.,Bergman, Jack,Makriyannis, Alexandros
, p. 10142 - 10157 (2014/01/17)
We report an approach for obtaining novel cannabinoid analogues with controllable deactivation and improved druggability. Our design involves the incorporation of a metabolically labile ester group at the 2′-position on a series of (-)-Δ8-THC a
KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
-
Page/Page column 78, (2011/10/31)
The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are a pharmaceutical composition and method of use thereof.
Controlled anion migrations with a mixed metal Li/K-TMP amide: General application to benzylic metalations
Fleming, Patricia,Oshea, Donal F.
supporting information; experimental part, p. 1698 - 1701 (2011/04/17)
A general method is described for benzylic metalation of o-, m-, and p-substituted toluenes using a mixed metal amide base generated from BuLi/KOtBu/TMP at -78 °C in THF. The excellent selectivity achieved can be rationalized by the ability of the mixed metal amide base to facilitate an anion migration from the kinetic (o-aryl) to the benzylic metalation site. Remarkably, this controlled anion migration is achievable with catalytic amounts of TMP at -78 °C.
Efficient synthesis of natural polyphenolic stilbenes: Resveratrol, piceatannol and oxyresveratrol
Sun, Hong-Yi,Xiao, Chun-Fen,Cai, Yu-Chen,Chen, Yu,Wei, Wen,Liu, Xian-Ke,Lv, Ze-Liang,Zou, Yong
experimental part, p. 1492 - 1496 (2010/12/25)
The practical synthesis of important natural polyphenolic stilbenes, including resveratrol, piceatannol and oxyresveratrol, through Perkin methodology is described. Starting from 3,5-dihydoxyacetophenone (1), the common intermediate 3,5-dimethoxyphenylacetic acid (3) can be obtained via methylation and Willgerodt-Kindler reaction. Perkin condensations between (3) and substituted phenylaldehydes 4 furnished E-2,3-diarylacrylic acids 5, followed by decarboxylation in Cu/quinoline giving stilbene intermediates 6 which bear the Z-configuration. Finally, through a simultaneous demethylation/isomerization process in AlI3/CH3CN system, the target compounds 7a-c can be obtained respectively in good to high overall yields. The synthetic method proved to be more concise, trans-specific, mild, economical and commonly applicable.
Total synthesis of Cytosporone B
Huang, He,Zhang, Lei,Zhang, Xiaodong,Ji, Xun,Ding, Xiao,Shen, Xu,Jiang, Hualiang,Liu, Hong
scheme or table, p. 1041 - 1043 (2010/10/19)
The total synthesis of Cytosporone B, a naturally occurring agonist for Nur77, has been accomplished. The key steps are the sequential Grignard reaction and Lemieux-van Rudloff oxidation followed by a deprotection of the methyl aromatic ether to phenol an
