7251-96-9Relevant academic research and scientific papers
Chemoinformatic-Guided Engineering of Polyketide Synthases
, p. 9896 - 9901 (2020)
Polyketide synthase (PKS) engineering is an attractive method to generate new molecules such as commodity, fine and specialty chemicals. A significant challenge is re-engineering a partially reductive PKS module to produce a saturated β-carbon through a r
Catalytic enantioselective nazarov cyclization: Construction of vicinal all-carbon-atom quaternary stereocenters
Jolit, Anais,Walleser, Patrick M.,Yap, Glenn P. A.,Tius, Marcus A.
supporting information, p. 6180 - 6183 (2014/06/23)
The diastereoselective asymmetric synthesis of vicinal all-carbon-atom quaternary stereocenters is a challenging problem in organic synthesis for which only few solutions have been described. A catalytic asymmetric Nazarov cyclization of fully substituted dienones that provides cyclopentenone derivatives with vicinal quaternary stereocenters in high optical purity and as single diastereoisomers is now reported.
Diastereospecific nazarov cyclization of fully substituted dienones: Generation of vicinal all-carbon-atom quaternary stereocenters
Jolit, Anais,Vazquez-Rodriguez, Saleta,Yap, Glenn P. A.,Tius, Marcus A.
supporting information, p. 11102 - 11105 (2013/10/22)
No vacancy: Fully substituted dienones that are highly polarized by a vinylogous carbonate group were found to undergo a remarkably rapid and diastereospecific Nazarov cyclization that led to cyclopentenones with vicinal all-carbon-atom quaternary centers (see example; SEM=2-(trimethylsilyl) ethoxymethyl, Tf=trifluoromethanesulfonyl). Copyright
BENZOXAZEPINES AS INHIBITORS OF P13K/MTOR AND METHODS OF THEIR USE AND MANUFACTURE
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Page/Page column 206, (2012/06/15)
The invention is directed 10 Compound's of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
Copper(II) triflate catalyzed amination and aziridination of 2-Alkyl substituted 1,3-dicarbonyl compounds
Ton, Thi My Uyen,Tejo, Ciputra,Tiong, Diane Ling Ying,Chan, Philip Wai Hong
experimental part, p. 7344 - 7350 (2012/06/16)
A method to prepare α-acyl-β-amino acid and 2,2-diacyl aziridine derivatives efficiently from Cu(OTf)2 + 1,10-phenanthroline (1,10-phen)-catalyzed amination and aziridination of 2-alkyl substituted 1,3-dicarbonyl compounds with PhI=NTs is described. By taking advantage of the orthogonal modes of reactivity of the substrate through slight modification of the reaction conditions, a divergence in product selectivity was observed. In the presence of 1.2 equiv of the iminoiodane, amination of the allylic C-H bond of the enolic form of the substrate, formed in situ through coordination to the Lewis acidic metal catalyst, was found to selectively occur and give the β-aminated adduct. On the other hand, increasing the amount of the nitrogen source from 1.2 to 2-3 equiv was discovered to result in preferential formal aziridination of the C-C bond of the 2-alkyl substituent of the starting material and formation of the aziridine product.
A double Mannich approach to the synthesis of substituted piperidones - Application to the synthesis of substituted E-ring analogues of methyllycaconitine
Chan, Yinman,Balle, Jared,Kevin Sparrow,Boyd, Peter D.W.,Brimble, Margaret A.,Barker, David
experimental part, p. 7179 - 7191 (2010/10/01)
The double Mannich reaction of acyclic α,γ-substituted β-keto esters and bis(aminol) ethers gives substituted 3,5-substituted-4- piperidones with high levels of diastereoselectivity. These piperdiones can be easily transformed into substituted E-ring analogues of the delphinium alkaloid methyllycacotine.
BENZOXAZEPINES BASED P13K/MT0R INHIBITORS AGAINST PROLIFERATIVE DISEASES
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Page/Page column 198, (2010/12/18)
The invention is directed to compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
The Reformatsky Reaction of 1-Acyl-3,5-dimethylpyrazoles. A Convenient Preparation of 4-Amino-3-oxoalkanoic Acid Derivatives
Kashima, Choji,Kita, Isanobu,Takahashi, Katsumi,Hosomi, Akira
, p. 723 - 726 (2007/10/02)
The conversion of N-acylpyrazoles into β-keto esters was accomplished efficiently by the treatment with α-bromo esters and zinc dust.Using this Reformatsky reaction of N-acylpyrazoles, 4-(protected amino)-3-oxoalkanoic acid derivatives were conveniently prepared as the key intermediates in the synthesis of statines.
