- Chemoinformatic-Guided Engineering of Polyketide Synthases
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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
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- Catalytic enantioselective nazarov cyclization: Construction of vicinal all-carbon-atom quaternary stereocenters
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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.
- Jolit, Anais,Walleser, Patrick M.,Yap, Glenn P. A.,Tius, Marcus A.
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supporting information
p. 6180 - 6183
(2014/06/23)
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- Diastereospecific nazarov cyclization of fully substituted dienones: Generation of vicinal all-carbon-atom quaternary stereocenters
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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
- Jolit, Anais,Vazquez-Rodriguez, Saleta,Yap, Glenn P. A.,Tius, Marcus A.
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supporting information
p. 11102 - 11105
(2013/10/22)
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- BENZOXAZEPINES AS INHIBITORS OF P13K/MTOR AND METHODS OF THEIR USE AND MANUFACTURE
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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.
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Page/Page column 206
(2012/06/15)
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- Copper(II) triflate catalyzed amination and aziridination of 2-Alkyl substituted 1,3-dicarbonyl compounds
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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.
- Ton, Thi My Uyen,Tejo, Ciputra,Tiong, Diane Ling Ying,Chan, Philip Wai Hong
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experimental part
p. 7344 - 7350
(2012/06/16)
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- BENZOXAZEPINES BASED P13K/MT0R INHIBITORS AGAINST PROLIFERATIVE DISEASES
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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.
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Page/Page column 198
(2010/12/18)
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- A double Mannich approach to the synthesis of substituted piperidones - Application to the synthesis of substituted E-ring analogues of methyllycaconitine
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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.
- Chan, Yinman,Balle, Jared,Kevin Sparrow,Boyd, Peter D.W.,Brimble, Margaret A.,Barker, David
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experimental part
p. 7179 - 7191
(2010/10/01)
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- The Reformatsky Reaction of 1-Acyl-3,5-dimethylpyrazoles. A Convenient Preparation of 4-Amino-3-oxoalkanoic Acid Derivatives
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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.
- Kashima, Choji,Kita, Isanobu,Takahashi, Katsumi,Hosomi, Akira
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p. 723 - 726
(2007/10/02)
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