122930-45-4Relevant academic research and scientific papers
Preparation of [6-isopropyl-4 - (4-fluoro phenyl) - 2-thio-5-yl] methyl ester
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Paragraph 0039-0040, (2018/01/19)
The invention relates to a preparation method of a pharmaceutical chemical intermediate and particularly relates to a preparation method of [6-isopropyl-4- (4-fluorophenyl)-2-thio-5-yl]formate. According to the method, p-fluorobenzaldehyde, isobutyryl ace
Synthesis of 2-substituted pyrimidines and benzoxazoles via a visible-light-driven organocatalytic aerobic oxidation: Enhancement of the reaction rate and selectivity by a base
Wang, Lin,Ma, Zhi-Gang,Wei, Xiao-Jing,Meng, Qing-Yuan,Yang, Deng-Tao,Du, Shao-Fu,Chen, Zi-Fei,Wu, Li-Zhu,Liu, Qiang
supporting information, p. 3752 - 3757 (2014/08/05)
An efficient visible-light-driven photocatalytic oxidation of various 2-substituted dihydropyrimidines and phenolic imines has been achieved using an organic photocatalyst eosin Y bis(tetrabutyl ammonium salt) (TBA-eosin Y) and inexpensive oxidant molecular oxygen. With the aid of a base, significantly enhanced photoinduced electron transfer from substrates dihydropyrimidines or phenolic imines to the excited state of TBA-eosin Y has enabled the aerobic oxidation to yield 2-(methylthio)pyrimidines or 2-arylbenzoxazoles selectively. This journal is the Partner Organisations 2014.
Synthesis of d3-cerivastatin for use as internal standard in a LC/MS/MS method developed for quantitation of the drug in human serum
Chen, Bang-Chi,Bednarz, Mark S.,Zhang, Huiping,Guo, Peng,Jemal, Mohammed,Robl, Jeffrey A.,Biller, Scott A.,Sundeen, Joseph E.,Balasubramanian, Balu,Barrish, Joel C.
, p. 311 - 319 (2007/10/03)
d3-Cerivastatin was synthesized as an internal standard for use in a LC/MS/MS method developed for the simultaneous quantitative determination of the drug in human serum. d3-Cerivastatin was efficiently prepared on large scale from d
Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors
Watanabe, Masamichi,Koike, Haruo,Ishiba, Teruyuki,Okada, Tetsuo,Seo, Shujiro,Hirai, Kentaro
, p. 437 - 444 (2007/10/03)
A novel series of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates were synthesized and evaluated for their ability to inhibit the enzyme HMG-CoA reductase in vitro. Monocalcium bis(+)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N- methanesulfonylaminopyrimidin)-5-yl]-(3R,5S)-dihydroxy- (E)-6-heptenoate (3a, S-4522) was selected as a candidate for further evaluation. Compound 3a was approximately four times more potent than lovastatin sodium salt (in inhibiting HMG-CoA reductase in vitro (IC50 = 11 nM). Compound 3a was shown to be the most potent cholesterol biosynthesis inhibitor in this series (IC50 = 1.12 nM) in rat isolated hepatocytes; its inhibitory activity was approximately 100 times more potent than pravastatin.
Synthesis of 1,3-Disubstituted-pyrroloisoquinoline-2-carboxylic Acids, Esters and Amides
Bridge, Andrew W.,Fenton, Garry,Halley, Frank,Hursthouse, Michael B.,Lehmann, Christian W.,Lythgoe, David J.
, p. 2761 - 2772 (2007/10/02)
A number of 1,3-disubstituted pyrroloisoquinoline-2-carboxylic esters have been prepared using a variety of independent routes.The corresponding acids and a range of amides were subsequently synthesised.The primary amides were found to differ significantly from those reported to arise from the reaction between the anion of an isoquinoline Reissert compound and an α,β-unsaturated nitrile.Re-investigation has established that the latter reaction does not produce primary amides.The true nature of the products as 2-acyl-3-aminopyrroloisoquinolines was established using X-ray crystallography.
Phosphorus-Containing Inhibitors of HMG-CoA Reductase. 2. Synthesis and Biological Activites of a Series of Substituted Pyrydynes Containing a Hydroxyphosphinyl Moiety
Robl, Jeffrey A.,Duncan, Laurelee A.,Pluscec, Jelka,Karanevsky, Donald S.,Gordon, Eric M.,et al.
, p. 2804 - 2815 (2007/10/02)
A series of 2,3,4,(5),6-substituted pyridines containing a hydroxyphosphinyl functionality have been prepared and were evaluated for their ability to inhibit the enzyme HMG-CoA reductase.Systematic substitution of both R1-R4 and X-Y
