29197-19-1Relevant academic research and scientific papers
Accelerating the optimization of enzyme-catalyzed synthesis conditionsviamachine learning and reactivity descriptors
Liang, Jinhu,Liu, Dongchang,Wan, Zhongyu,Wang, Quan-De
supporting information, p. 6267 - 6273 (2021/07/28)
Enzyme-catalyzed synthesis reactions are of crucial importance for a wide range of applications. An accurate and rapid selection of optimal synthesis conditions is crucial and challenging for both human knowledge and computer predictions. In this work, a
Enantioselective Synthesis of 2,3-Dihydrofurans via Ammonium Ylides
Worgull, Dennis,?hler, Laura,Strache, Joss Pepe,Friedrichs, Teresa,Ullrich, Patrick
supporting information, p. 6077 - 6080 (2017/11/14)
A chiral, ammonium ylide based access to tetrasubstituted 2,3-dihydrofurans starting from readily available benzylidene dicarbonyls and bromo acetophenones has been developed. The products are obtained in moderate to good yields with excellent diasteroselectivity and good to excellent enantioselectivity (up to 99:1 e.r.). The employed chiral amine can be recovered in near quantitative yield. The transformation can be run as a three-component one-pot reaction, generating the ammonium salt and ylide in situ. The scope of this reaction includes 17 new dihydrofurans with aromatic or heteroaromatic substituents.
Knoevenagel condensation of aromatic aldehydes with active methylene compounds catalyzed by lipoprotein lipase
Ding, Yan,Ni, Xiao,Gu, Mengjie,Li, Shuang,Huang, He,Hu, Yi
, p. 101 - 104 (2015/02/19)
A screening of using different lipases to catalyze the Knoevenagel reaction was realized, and lipase lipoprotein (LPL) from Aspergillus niger showed the best catalytic performance. The reaction conditions including solvent, enzyme loading, and temperature were screened to improve the reaction efficiency. Various kinds of substrates were investigated, and almost all the target products were obtained in good to excellent yields (76-98%) with Z configuration exclusively. This procedure provides a novel, green and efficient method for the Knoevenagel condensation of aromatic aldehydes with active methylene compounds.
One-pot, three-component approach to the synthesis of 3,4,5-trisubstituted pyrazoles
Kamal, Ahmed,Sastry, K. N. Visweswara,Chandrasekhar,Mani, Geeta Sai,Adiyala, Praveen Reddy,Nanubolu, Jagadeesh Babu,Singarapu, Kiran Kumar,Maurya, Ram Awatar
, p. 4325 - 4335 (2015/05/13)
An operationally simple and high yielding protocol for the synthesis of polyfunctional pyrazoles has been developed through one-pot, three-component coupling of aldehydes, 1,3-dicarbonyls, and diazo compounds as well as tosyl hydrazones. The reaction proceeds through a tandem Knoevenagel condensation, 1,3-dipolar cycloaddition, and transition metal-free oxidative aromatization reaction sequence utilizing molecular oxygen as a green oxidant. The scope of the reaction was studied by varying the aldehyde, 1,3-dicarbonyl, and diazo component individually.
A facile synthesis of trisubstituted alkenes from β-diketones and aldehydes with AlCl3 as catalyst
Li, Zheng-Nan,Chen, Xiao-Liang,Fu, Yu-Jie,Wang, Wei,Luo, Meng
experimental part, p. 25 - 35 (2012/05/20)
Preparation of trisubstituted alkenes from low-activity β-diketones and aldehydes with aluminum chloride as catalyst has been studied. The frequently used catalyst AlCl3 is used for the first time to promote this condensation. The procedure is a convenient, low toxicity, and highly efficient method for industrial synthesis of trisubstituted alkenes in high yield. Springer Science+Business Media B.V. 2011.
Magnesium perchlorate as efficient Lewis acid for the Knoevenagel condensation between β-diketones and aldehydes
Bartoli, Giuseppe,Bosco, Marcella,Carlone, Armando,Dalpozzo, Renato,Galzerano, Patrizia,Melchiorre, Paolo,Sambri, Letizia
, p. 2555 - 2557 (2008/09/21)
A new protocol for the Knoevenagel condensation between β-diketones and aliphatic and aromatic aldehydes promoted by Mg(ClO4)2 under mild conditions is reported.
Synthesis of some new unsymmetrically substituted 1,4-dihydropyridines
Memarian, Hamid R.,Abdoli-Senejani, Masumeh,D?pp, Dietrich
, p. 50 - 56 (2008/02/10)
A series of some new 3,5-unsymmetrically substituted 1,4-dihydropyridines have been synthesized, which have ethoxycarbonyl and acetyl groups on 3- and 5-positions, respectively. A three-step procedure has been examined to increase the yield of the desired products, by suppressing the formation of the symmetrically substituted 3,5-diacetyl-1,4-dihydropyridines and 3,5-diethoxycarbonyl-1,4-dihydropyridines.
Studies on cerebral protective agents. I. Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities
Kuno,Sugiyama,Katsuta,Kamitani,Takasugi
, p. 1452 - 1461 (2007/10/02)
Novel 4-arylpyrimidine derivatives were synthesized by the oxidation of 4-aryl-1,4-dihydropyrimidines, and their effects on anti-anoxic (AA) activity in mice and anti-lipid peroxidation (ALP) activity in rat brain mitochondria were investigated. Among these compounds, ethyl 6-methyl-2-phenyl-4-(4-pyridyl)-5-pyrimidinecarboxylate (4b) has AA activity (10mg/kg, i.p.) and ethyl 6-methyl-4-(3-nitrophenyl)-2-phenyl-5-pyrimidinecarboxylate (4f) has ALP activity (73% inhibition at 10-5 g/ml). The latter compound (100mg/kg, i.p.) was also effective on arachidonate-induced cerebral edema in rats with comparable potency to that of vitamin E.
Substituted beta-diketones and their use
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, (2008/06/13)
Compounds of formula wherein n is 0 or 1, R1 and R2 are independently methyl, ethyl or cyclopropyl and R is an optionally substituted phenyl or heteroaryl group or salt or ester thereof are useful in the treatment of inflammatory bowel disease.
