synthetic strategy
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Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 535
Wong Pooi Wen Kathy ◽  
Li Lin Ong ◽  
Surabhi Devaraj ◽  
Duc Thinh Khong ◽  
Zaher M. A. Judeh

In this study, we report on an orthogonal strategy for the precise synthesis of 3,3′-, 3,4′-, and 3,6′-phenylpropanoid sucrose esters (PSEs). The strategy relies on carefully selected protecting groups and deprotecting agents, taking into consideration the reactivity of the four free hydroxyl groups of the key starting material: di-isopropylidene sucrose 2. The synthetic strategy is general, and potentially applies to the preparation of many natural and unnatural PSEs, especially those substituted at 3-, 3′-, 4′- and 6′-positions of PSEs.

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 463
Luca Pozzetti ◽  
Roberta Ibba ◽  
Sara Rossi ◽  
Orazio Taglialatela-Scafati ◽  
Donatella Taramelli ◽  

The potential of natural and synthetic chalcones as therapeutic leads against different pathological conditions has been investigated for several years, and this class of compounds emerged as a privileged chemotype due to its interesting anti-inflammatory, antimicrobial, antiviral, and anticancer properties. The objective of our study was to contribute to the investigation of this class of natural products as anti-leishmanial agents. We aimed at investigating the structure–activity relationships of the natural chalcone lophirone E, characterized by the presence of benzofuran B-ring, and analogues on anti-leishmania activity. Here we describe an effective synthetic strategy for the preparation of the natural chalcone lophirone E and its application to the synthesis of a small set of chalcones bearing different substitution patterns at both the A and heterocyclic B rings. The resulting compounds were investigated for their activity against Leishmania infantum promastigotes disclosing derivatives 1 and 28a,b as those endowed with the most interesting activities (IC50 = 15.3, 27.2, 15.9 μM, respectively). The synthetic approaches here described and the early SAR investigations highlighted the potential of this class of compounds as antiparasitic hits, making this study worthy of further investigation.

Synlett ◽  
2022 ◽  
Qing Li ◽  
Qi Wang ◽  
Yuan Yuan ◽  
Yulan Chen

Quantitative and real-time characterization of mechanically induced bond scission events taken place in polymeric hydrogels is essential to uncover their fracture mechanics. Herein, a class of mechanochemiluminescent swelling hydrogels have been synthesized through a facile micellar copolymerization method using chemiluminescent bis(adamantyl)-1,2-dioxetane (Ad) as a crosslinker. This design and synthetic strategy ensure intense mechanochemiluminescence from Ad located in a hydrophobic network inside micelles. Moreover, the mechanochemiluminescent colors can be tailored from blue to red by mixing variant acceptors. Taking advantages of the transient nature of dioxetane chemiluminescence, the damage distribution and crack evolution of the hydrogels can be visualized and analyzed with high spatial and temporal resolution. The results demonstrate the strengths of the Ad mechanophore and micellar copolymerization method in the study of damage evolution and fracture mechanism of swelling hydrogels.

Synthesis ◽  
2022 ◽  
Kento Iwai ◽  
Haruka Yamauchi ◽  
Soichi Yokoyama ◽  
Nagatoshi Nishiwaki

Many biologically active nicotinonitriles have been reported to date. Consequently, the development of synthetic methods for multiply arylated/alkylated nicotinonitriles remains a sought-after field of research. In the present work, a new synthetic strategy for multi-substituted nicotinonitriles was provided. A FeCl3-promoted condensation-cyclization reaction of an enamino nitrile and α,β-unsaturated ketones efficiently proceeded with a wide range of substrates. It is noteworthy that this method facilitated the access to fully- and differently substituted nicotinonitriles including tetra-arylated nicotinonitriles in only three steps. Using the functionality of the cyano group, the copper-catalyzed annulation reaction of the nicotinonitrile was achieved to yield benzo[c][2,7]naphthyridin-5(6H)-one.

RSC Advances ◽  
2022 ◽  
Vol 12 (1) ◽  
pp. 251-264
Ko-Hua Yu ◽  
Hsin-Yi Hung

Since 1994, YC-1 (Lificiguat) has been synthesized, and many targets for special bioactivities have been explored, such as stimulation of platelet-soluble guanylate cyclase, indirect elevation of platelet cGMP levels, and inhibition of HIF-1 and NF-κB.

2022 ◽  
Pol Gimeno-Fonquernie ◽  
W Liang ◽  
Jorge Albalad ◽  
Andrew Kuznicki ◽  
Jason Price ◽  

Metal-organic layers (MOLs) are of great interest in heterogeneous catalysis, particularly those that can accommodate extraneous metal centres. Here, we demonstrate a two-step preorganisation/delamination synthetic strategy using CuI as a...

2022 ◽  
Wang Xia ◽  
Zi-An Zhou ◽  
Jie Lv ◽  
Shao-Hua Xiang ◽  
Yong-Bin Wang ◽  

N-aryl phenothiazines and phenoxazines are of significant importance in various disciplines throughout academia and industry. Conventional synthetic strategy for the construction of these structures centers on transition-metal-catalyzed cross-coupling of aryl...

Nanoscale ◽  
2022 ◽  
Ignacio Rosa-Pardo ◽  
Rita Belen Cevallos-Toledo ◽  
Lakshminarayana Polavarapu ◽  
Raul Arenal ◽  
Raquel E. Galian ◽  

The long-standing debate about the morphology of colloidal methylammonium lead bromide perovskites nanocrystals, manufactured by our nontemplate synthetic strategy reported in 2014, is now resolved; specifically, the highest green emissive...

2022 ◽  
Juan Li ◽  
Chengdong Liu ◽  
Xiang Wang ◽  
Yayun Ding ◽  
Zhou Wu ◽  

Incorporating transition metal (TM) complexes into cluster-based chalcogenide frameworks is an effective synthetic strategy to induce structural diversity and to control the optoelectronic properties, which may further improve their photocatalytic...

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