- Non-metal Lewis acid-catalyzed cross-Claisen condensation for β-keto esters
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In this work, we disclose a new catalytic and highly chemoselective cross-Claisen condensation of esters. In the presence of TBSNTf2 as a non-metal Lewis acid, various esters can undergo cross-Claisen condensation to form β-keto esters which are important building blocks. Compared with the traditional Claisen condensation, this process, employing silyl ketene acetals (SKAs) as carbonic nucleophiles to achieve cross-Claisen condensation, requires mild conditions and has good tolerance of functional groups. This journal is
- Han, Zhengyu,Huang, Hai,Meng, Fuliang,Yang, Zhenkun,Zhang, Tianyu,Zhou, Dapeng
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supporting information
p. 9163 - 9166
(2021/11/16)
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- 6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H
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Human immunodeficiency virus (HIV) reverse transcriptase (RT)-associated ribonuclease H (RNase H) remains an unvalidated drug target. Reported HIV RNase H inhibitors generally lack significant antiviral activity. We report herein the design, synthesis, biochemical and antiviral evaluations of a new 6-biphenylmethyl subtype of the 3-hydroxypyrimidine-2,4-dione (HPD) chemotype. In biochemical assays, analogues of this new subtype potently inhibited RT RNase H in low nanomolar range without inhibiting RT polymerase (pol) or integrase strand transfer (INST) at the highest concentrations tested. In cell-based assays, a few analogues inhibited HIV in low micromolar range without cytotoxicity at concentrations up to 100 μM.
- Wang, Lei,Tang, Jing,Huber, Andrew D.,Casey, Mary C.,Kirby, Karen A.,Wilson, Daniel J.,Kankanala, Jayakanth,Parniak, Michael A.,Sarafianos, Stefan G.,Wang, Zhengqiang
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supporting information
p. 680 - 691
(2018/07/29)
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- SUBSTITUTED AMINO-COMPOUNDS AND USES THEREOF
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This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provi
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Page/Page column 84-85; 130
(2008/06/13)
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- SUBSTITUTED AMINO-PYRIMIDONES AND USES THEREOF
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This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia,Ib), and their phatmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Abeta related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
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Page/Page column 98-99; 144-145
(2008/06/13)
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- The diazo route to diazonamide A. Studies on the indole bis-oxazole fragment
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Various approaches to the indole bis-oxazole fragment of the marine secondary metabolite diazonamide A are described, all of which feature dirhodium(II)-catalyzed reactions of diazocarbonyl compounds in key steps. Thus, 3-bromophenylacetaldehyde is conver
- Davies, James R.,Kane, Peter D.,Moody, Christopher J.
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p. 7305 - 7316
(2007/10/03)
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