259529-54-9Relevant academic research and scientific papers
Diastereoselective Copper-Mediated Conjugate Addition of Functionalized Magnesiates for the Preparation of Bisaryl Nrf2 Activators
Glogowski, Michal P.,Matthews, Jay M.,Lawhorn, Brian G.,Minbiole, Kevin P. C.
, p. 3120 - 3137 (2021/03/01)
A two-step metal-halogen exchange and diastereoselective copper-mediated Michael addition onto a complex α,β-unsaturated system has been developed and applied toward the synthesis of bisaryl Nrf2 activators. Optimization of metal-halogen exchange using (n
Preparation method of ezetimibe intermediate
-
Paragraph 0052; 0053; 0054; 0055, (2016/11/14)
The invention discloses a preparation method of an ezetimibe intermediate. The intermediate is (S)-1-(4-fluorophenyl)-5-(2-oxo-phenyloxazolidinyl-3-yl)pentane-1, 5-dione. The preparation method comprises that 1-(4-fluorophenyl)ethanone and a silane protective agent undergo a reaction to produce ((1-(4-fluorophenyl)vinyl)oxo)trimethylsilane, (S)-4-phenyloxazolidin-2-one and acryloyl chloride undergo a condensation reaction to produce (S)-3-acrylyl-4-phenyloxazolidin-2-one, and the ((1-(4-fluorophenyl)vinyl)oxo)trimethylsilane and the (S)-3-acrylyl-4-phenyloxazolidin-2-one undergo a condensation reaction to produce the ezetimibe intermediate. The preparation method utilizes a convergent type route, has the total yield of 80% or more, utilizes cheap and easily available raw materials, utilizes less types of solvents, produces small toxicity, has a short production period, utilizes simple production units operated easily, is safe and environmentally friendly and is very suitable for industrial production.
Straightforward and facile synthesis of a bioactive component from zingiber cassumunar ROXB.
Fang, Yuanying,Yang, Zunhua,Park, Haeil
supporting information, p. 1212 - 1217 (2014/04/17)
Straightforward and facile synthesis of a bioactive component A from Zingiber cassumunarRoxb. is described. The phenylbutenoid dimer A was reported to possess anti-inflammatory and cytotoxic activities. The optically active cyclohexene ring fragment was o
Synthetic studies of cyclic peptides stephanotic acid methyl ester, celogentin C, and moroidin
Li, Lei,Hu, Weimin,Jia, Yanxing
, p. 7753 - 7762 (2014/12/10)
An account of the total synthesis of stephanotic acid methyl ester and celogentin C is presented. The present synthesis features a tandem asymmetric Michael addition/bromination sequence for the synthesis of leucine-tryptophan moiety, and an oxidative coupling reaction to form the tryptophan-imidazole linkage. Moreover, the total synthesis of moroidin had also been studied, and three different synthetic strategies for the construction of the right-hand ring of moroidin were studied.
Diastereoselective aziridination of chiral electron-deficient olefins with N-chloro-N-sodiocarbamates catalyzed by chiral quaternary ammonium salts
Murakami, Yuta,Takeda, Youhei,Minakata, Satoshi
experimental part, p. 6277 - 6285 (2011/10/02)
Chiral quaternary ammonium salt-catalyzed diastereoselective aziridination of electron-deficient olefins that possess a chiral auxiliary with N-chloro-N-sodiocarbamates was developed. The key to high stereoselectivity was found to be the employment of the
Copper-catalysed domino silylative aldol reaction leading to stereocontrolled chiral quaternary carbons
Welle, Alexandre,Petrignet, Julien,Tinant, Bernard,Wouters, Johan,Riant, Olivier
supporting information; experimental part, p. 10980 - 10983 (2010/11/21)
(Chemical Equation Presented) Asymmetric aldol reaction: A domino silylation-aldol reaction between enoyloxazolidinones and various aldehydes has been developed (see scheme). The process catalysed by a copper complex in the presence of a borosilane led to high diastereoselectivities. Yields between 59 and 90 % and d.r. values between 78:22 to 95:5 were obtained. When methacryloyloxazolidinones were used, a controlled chiral quaternary carbon was generated. BPin=4,4,5,5-tetramethyl-1,3,2dioxaborolan-2-yl.
Nitrile Ylides: Diastereoselective cycloadditions using chiral oxzolidinones without Lewis acid
Mukund P, Sibi,Soeta, Takahlro,Jasperse, Craig P.
supporting information; experimental part, p. 5366 - 5369 (2010/02/28)
"Chemical Equation Presented" Lewis acid complexation Is generally required for chiral-auxiliary-controlled stereoselectivity, and chiral Lewis acid catalysis Is frequently optimal for Introducing asymmetry. In this work, we show that nitrlle ylide cycloadditions to electron-poor acceptors attached to chiral auxiliaries proceed In high yield and stereoselectivity in the absence of Lewis acids. In contrast, chiral Lewis acids are Inferior In these cycloadditions.
2-OXAZOLIDINONES AND THEIR USE AS INHIBITORS OF ANIMAL CELL MOTILITY AND GROWTH
-
Page 53; 67, (2010/11/30)
Cell motility and growth inhibitors, including compounds of the general structural formula (I), and use of the cell motility and cell growth inhibitors, and pharmaceutically acceptable salts, pro-drugs, and solvates thereof, as therapeutic agents, are disclosed.
Olefin Metathesis in the Design and Synthesis of a Globally Constrained Grb2 SH2 Domain Inhibitor
Gao, Yang,Wei, Chang-Qing,Burke Jr., Terrence R.
, p. 1617 - 1620 (2007/10/03)
(matrix presented) One drawback frequently associated with olefin metathesis-mediated peptide macrocyclization, the loss of side chain functionality at sites of ring closure, may be circumvented by incorporation of side chain functionality within the ring
