86768-23-2Relevant academic research and scientific papers
A one-pot approach to ethyl 1,4,5-triaryl-1H-pyrazole-3-carboxylates via an improved claisen condensation-knorr reaction sequence
Zhai, Jiaojiao,Gu, Chunhui,Jiang, Jianan,Zhang, Shunli,Liao, Daohua,Wang, Lei,Zhu, Dunru,Ji, Yafei
supporting information, p. 1526 - 1538 (2014/01/06)
A one-pot approach to ethyl 1,4,5-triaryl-1H-pyrazole-3-carboxylates has been developed in moderate to high yields. The tert-BuOLi-mediated Claisen condensation of 1,2-diarylethanones and ethyl oxalyl chloride efficiently provided the enolized lithium salts of ethyl 2,4-dioxo-3,4-diarylbutanoates, which in situ reacted with arylhydrazine hydrochlorides via a hydrochloric acid-promoted Knorr reaction to produce the exquisite triarylpyrazole-3- carboxylates. The procedure promises a convenient access to this highly crowded framework for drug discovery. Copyright
Synthesis of the pyrazole isostere of valdecoxib
Szabo,Fischer,Kis-Varga
, p. 522 - 524 (2007/10/03)
4-(5-Methyl-3-phenyl-1H-pyrazole-4-yl)-benzenesulfonamide, the pyrazole isostere of valdecoxib was synthesised. The title compound was prepared by a six-step procedure starting from commercially available deoxybenzoin 1. The pyrazole isostere 13 showed sl
Polyfunctional (R)-2-Hydroxycarboxylic Acids by Reduction of 2-Oxo Acids with Hydrogen Gas or Formate and Resting Cells of Proteus vulgaris
Schummer, Anita,Yu, Hongtao,Simon, Helmut
, p. 9019 - 9034 (2007/10/02)
Various (R)-2-hydroxy acids such as (R)-2-hydroxy-3-enoic-, 3,5-dienoic-, 4-oxo-, (R,S)-3-hydroxy and some others were prepared on a scale up to 0.12 mol by biocatalytic reduction of the corresponding 2-oxo acids with P. vulgaris and hydrogen gas and/or formate as electron donors.With the exception of the 2-hydroxy-4-oxo acids it could be proved that the enantiomeric excess is >97 percent.For the 4-oxo derivatives this enantiomeric excess can be assumed.The yields of isolated products are high because they were isolated from rather small amounts of biocatalyst and low buffer concentrations.Product concentrations in the range of 0.1- 0.24 M were obtained.For 1 mmol of product formation in 15-20 h about 20-40 mg (dry weight) of P. vulgaris cells are necessary.
