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| 1 | Photocatalytic decarboxylative coupling between α-oxocarboxylicacids and alkenes显示文摘Photocatalytic decarboxylative cross-coupling which achieves the derivatization of widespread organic acids has become a hot topic in organic synthesis.As special acids,α-oxocarboxylicacids show the great potential in running decarboxylation to construct ketone derivatives.In this article,we have developed a photocatalytic decarboxylative cross-coupling ofα-oxocarboxylic acids and olefins to the synthesis of diverse aryl ketones.Various alkenes andα-oxocarboxylicacids were compatible,generating the desired products in up to 90%yield.Preliminary mechanism studies suggest that a free radical pathway is involved in this process. | Ziyue Chen Fangling Lu Feng Yuan Juanjuan Sun Linyu Du Zhen Li Meng Gao Renyi Shi Aiwen Lei | 2019 | Science China Chemistry2019，62，11： | 2 |
| 2 | Cytotoxic and antibacterial polyketide-indole hybrids synthesized from indole-3-carbinol by Daldinia eschscholzii显示文摘Two skeletally undescribed polyketide-indole hybrids(PIHs), named indolchromins A and B,were generated from indole-3-carbinol(I3 C) in the fungal culture(Daldinia eschscholzii). The indolchromin structures were elucidated mainly by their 1 D and 2 D NMR spectra with the former confirmed by the single-crystal X-ray crystallographic analysis. Each indolchromin alkaloid was chirally separated into four isomers, whose absolute configurations were assigned by comparing the recorded circular dichroism(CD) spectra with the electronic CD(ECD) curves computed for all optional stereoisomers. Furthermore, the indolchromin construction pathways in fungal culture were clarified through enzyme inhibition, precursor feeding experiment, and energy calculation. The cascade reactions,including decarboxylative Claisen condensation catalyzed by 8-amino-7-oxononanoate synthase(AONS),C(sp3)-H activation, double bond migration, and Michael addition, all undergone compatibly during the fungal cultivation. In an MIC range of 1.3–8.6 μmol/L,(2 S,4 R)-and(2 R,4 S)-indolchromin A and(2 R,4 S)-indolchromin B are inhibitory against Clostridium perfringens, Clostridium difficile, Veillonella sp.,Bacteroides fragilis, and Streptococcus pyogenes.(2 R,4 S)-Indolchromin A and(2 S,4 S)-indolchromin B were cytotoxic against the human breast cancer cell line MDA-MB-231 with IC50 values of 27.9 and131.2 nmol/L, respectively, with the former additionally active against another human breast cancer cell line MCF-7(IC_(50)94.4 nmol/L). | Liping Lin Nan Jiang Huimin Wu Yaning Mei Jie Yang Renxiang Tan | 2019 | Acta Pharmaceutica Sinica B2019，9，2： | 1 |
| 3 | Synthesis, Structure and Decarboxylative Behavior of a Nitro-coordinated Potassium Compound显示文摘A novel nitro-coordinated potassium compound [K(Htdc)(H_2O)]_n(tdc = 3-nitro-thiophene-2,5-dicarboxylate), has been synthesized and characterized. The complex with a two-dimensional(2D) layer structure contains an infinite K-O ladder-shaped chain, which is connected through carboxyl and unusual nitro-coordination of Htdc– anion. Then the 2D layers are further extended by intermolecular hydrogen-bonding to form a three-dimensional(3D) supramoleculalr network. Variable temperature powder X-ray diffractions, thermogravimetric analysis and nuclear magnetic resonance studies exhibit that the compound has a thermal-induced decarboxylative behavior. | 李东密 崔佳佳 姚佳欣 李召好 赵邦屯 | 2019 | Chinese Journal of Structural Chemistry2019，38，3： | 0 |
| 4 | A new synthesis of A-nor-△^(3(5),9(10)) estradiene-2,17-dione显示文摘A-nor-Δ3(5),9(10)-estradiene-2,17-dione 1,a potential precursor for synthesis of some new steroidalcontraceptives,was synthesized from 3β-hydroxy-5α-chloro-6β,19-epoxy-androstane-17-one 6 as the sterting mater al,which is the key intermediate of steroidal contraceptive of norethindrone,in an overall yield of 25% in 5 steps through the sequence of 5 reactions:(i) oxidative dccyclization,(ii) decarhoxylative cyclization,(iii) reductive decy clization,(iv) dehydroxy methylation,(v) | 周向东 周维善 王钟麒 | 1997 | Science China Chemistry1997，40，3： | 0 |
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