Review
Chemistry, Applied
Yudha P. Budiman, Stephen A. Westcott, Udo Radius, Todd B. Marder
Summary: Organoboron compounds are essential building blocks for organic reactions, with recent focus on the synthesis of fluorinated aryl boronic acid derivatives. However, instability issues arise under basic conditions, particularly accelerated in compounds with an ortho-fluorine group, leading to protodeboronation. Research is aimed at developing novel synthesis methodologies to avoid such issues.
ADVANCED SYNTHESIS & CATALYSIS
(2021)
Article
Chemistry, Multidisciplinary
Masahiko Seki, Sandeep Ramesharao Tapkir, Maheshwara Reddy Nadiveedhi, Shaheen Kasim Mulani, Kazushi Mashima
Summary: Diarylmethanes, crucial building blocks for SGLT2 inhibitors, were synthesized via ketone synthesis by Friedel-Crafts acylation with TiCl4, followed by reduction with TiCl4/NaBH4. This newly developed protocol offers a cleaner and more efficient method compared to previous approaches using AlCl3 and BF3 center dot OEt2/Et3SiH, allowing for the expedient and cost-effective synthesis of diarylmethanes corresponding to canagliflozin, empagliflozin, and luseogliflozin. In the case of dapagliflozin synthesis, an alternative reduction method using InCl3/Al/BF3 center dot OEt2 was employed.
Review
Biochemistry & Molecular Biology
Yuta Murai, Makoto Hashimoto
Summary: In the fields of materials science and medicinal chemistry, heteroaromatic derivatives are important in developing new devices and discovering drugs. (3-trifluoromethyl)phenyldiazirine (TPD) is a crucial chemical method for understanding biological processes. TPD has been widely used in materials science to create novel electric and polymer devices at a lower cost. The combination of heteroaromatics and (3-trifluoromethyl)diazirine is a promising option for creating better materials and understanding the mechanisms of bioactive heteroaromatic compounds. This review provides a comprehensive synthesis of (3-trifluoromethyl)diazirine-substituted heteroaromatics.
Review
Chemistry, Multidisciplinary
Maxim Golfmann, Johannes C. L. Walker
Summary: Bicyclobutanes, highly strained isolable organic compounds, have attracted a lot of attention in organic chemistry due to their low reactivity. In recent years, creative synthetic strategies have been developed to exploit their reactivity, leading to the synthesis of more practical routes. The weak central C-C bond in bicyclobutanes has been utilized in various addition, rearrangement and insertion reactions, offering quick access to complex molecular scaffolds. This review provides an overview of different options for bicyclobutane synthesis, the compounds that can be prepared from bicyclobutanes, and the associated modes of reactivity.
COMMUNICATIONS CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yuliana Zabolotna, Dmitriy M. Volochnyuk, Sergey V. Ryabukhin, Dragos Horvath, Konstantin S. Gavrilenko, Gilles Marcou, Yurii S. Moroz, Oleksandr Oksiuta, Alexandre Varnek
Summary: Efficient synthesis of desired compounds is crucial for chemical space exploration in drug discovery, which is influenced by both established synthetic protocols and the availability of corresponding building blocks (BBs). This study analyzes the chemical space of 400,000 purchasable BBs, examining their physicochemical properties and diversity to assess their coverage of medicinal chemistry needs. The analysis is based on a universal topographic map that visualizes libraries and their differences in coverage.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2022)
Article
Chemistry, Multidisciplinary
Joshua L. Clark, Rifahath M. Neyyappadath, Cihang Yu, Alexandra M. Z. Slawin, David B. Cordes, David O'Hagan
Summary: This study introduces monoalkylated derivatives containing the polar all-cis 2,3,4,5,6-pentafluorocyclohexyl (Janus face) motif, and demonstrates their conversion to various compounds, including representative members of antiviral compounds.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Chemistry, Multidisciplinary
Shaomin Chen, Luigi Vaccaro, Yanlong Gu
Summary: Diversity-oriented synthesis is a powerful tool for constructing complex structures using versatile reagents. Simple and practical versatile reagents with multiple reactivities are preferred for practical and universal applications. These reagents can play different roles simultaneously in the same reaction, offering more possibilities for synthesizing active pharmaceutical ingredients.
CHINESE CHEMICAL LETTERS
(2024)
Article
Chemistry, Applied
Kossi Efouako Soklou, Hamid Marzag, Beatrice Vallee, Sylvain Routier, Karen Ple
Summary: Gold(I) catalysis was used for the intramolecular cyclization of tertiary alcohols with terminal alkynes to form diverse aza-spirocycles. The reaction produced both sulfonylated and acylated spirocyclic nitrogen derivatives, demonstrating the robustness of the method. These compounds were then incorporated into biologically relevant scaffolds to give the first selective spirocyclic inhibitors of LIMK1.
ADVANCED SYNTHESIS & CATALYSIS
(2022)
Article
Chemistry, Organic
Yongan Liu, Qijun Pan, Xiaojun Hu, Yong Guo, Qing-Yun Chen, Chao Liu
Summary: In this study, a practical and efficient copper-catalyzed method was reported for the conversion of various arenediazonium salts to N-protected sulfonimidoyl fluorides. This protocol tolerates a wide range of functional groups and is suitable for late-stage modification of complex bioactive molecules, leading to the synthesis of pharmaceutically important primary sulfonamides and sulfonimidamides in minimal synthetic steps.
Article
Chemistry, Organic
Eagala Ramesh, Laxman D. Nandawadekar, Ramana Sreenivasa Rao, D. Srinivasa Reddy
Summary: A simple and efficient two-step method for the synthesis of silacyclohexanones using TosMIC is presented. The prepared silacyclohexanones were transformed into various heterocycles with silicon incorporation. Additionally, the method was successfully applied to the synthesis of a sila analogue of the HDAC6 inhibitor tubastatin A.
Article
Chemistry, Organic
Yang Chao, Muthusamy Subramaniam, Kayambu Namitharan, Yumei Zhu, Victor Koolma, Zitong Hao, Shikang Li, Yaxin Wang, Ilyos Hudoynazarov, Fedor M. Miloserdov, Han Zuilhof
Summary: In this study, the first asymmetric synthesis of large chiral macrocycles with chiral sulfur atoms is reported. The method utilizes efficient building blocks with two chiral sulfur centers and diphenols to form novel S-O bonds through stereospecific SuFEx and SuPhenEx click chemistries. The characteristic results include the enantiospecific one-step synthesis of rings consisting of 21-58 members and the characterization of both enantiomers (R,R and S,S) using X-ray crystallography.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Ulrich Luecking
Summary: This article highlights the emerging trends and opportunities for drug designers to utilize the sulfoximine group in medicinal chemistry, such as in the construction of complex molecules, PROTACs, ADCs, and novel warheads for covalent inhibition. Despite the increasing interest in the sulfoximine group in recent years, there is still ample room for further innovative applications.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Chemistry, Organic
Lei Chen, Yuan Yang, Fei Li, Fei Jin, Bin He, Jun Yang
Summary: This study presents a novel synthetic route for producing a stable and versatile cyclopropene precursor, addressing the challenges related to instability and difficulties in scale-up processes. The cyclopropene precursor enables the easy synthesis of various cyclopropenes with different functional groups and handles. Among the synthesized cyclopropene derivatives, the 1-methylcyclopropene uracil nucleoside derivative 40 exhibited the highest second-order kinetic constant when reacting with the 5-TAMRA-Tz fluorescent dye.
ORGANIC CHEMISTRY FRONTIERS
(2023)
Article
Chemistry, Multidisciplinary
Jan H. Griwatz, Mika L. Kessler, Hermann A. Wegner
Summary: The synthesis of [n]cycloparaphenylenes ([n]CPPs) and similar nanohoops relies on combining building blocks to a macrocyclic precursor, followed by aromatization. Access to large amounts of these building blocks simplifies the synthesis and research of CPPs as novel functional materials. In this study, we demonstrate a continuous-flow synthesis of key CPP building blocks using self-built reactors on up to kilogram scale. This fast and large-scale access provides new possibilities for further research in the field of curved aromatic compounds.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Physical
De-Li Ma, Cheng Qian, Qiao-Yan Qi, Zhong-Ri Zhong, Guo-Fang Jiang, Xin Zhao
Summary: The principle of reticular chemistry is widely used in designing crystalline porous materials like MOFs and COFs. Recent research has shown that the connecting sequence of building blocks plays a crucial role in determining the crystalline structures of COFs. The article establishes a model system to demonstrate the impact of different connecting sequences on COFs structures and verifies it through target synthesis.
Article
Computer Science, Software Engineering
Rong Lu, Zeyu Yang, Chuyi Gao, Maolong Xi, Yang Zhang, Jian Xiong, Chi-Man Pun, Hao Gao
Summary: This study introduces a new ABC algorithm with an elite search strategy to accelerate convergence speed and improve local search ability. Experimental results show better performance in comparison with other state of the art algorithms in image segmentation problem of mechanical robot vision systems.
CONCURRENCY AND COMPUTATION-PRACTICE & EXPERIENCE
(2021)
Review
Surgery
Chenglong Wang, Wenwen Huang, Yingdan Gu, Jian Xiong, Zhuomiao Ye, Dong Yin, Xiaoping Mu
Summary: The study revealed a significant association between urinary tract infection (UTI) and prosthetic joint infection (PJI) after joint arthroplasty, supporting the theory of PJI occurring via a haematogenous route from the genitourinary tract harboring bacteria in UTI. Postponing surgery and treating patients with known UTI preoperatively are recommended based on the findings.
SURGEON-JOURNAL OF THE ROYAL COLLEGES OF SURGEONS OF EDINBURGH AND IRELAND
(2021)
Review
Nursing
Jian Xiong, Mingzhu Ye, Lecong Wang, Guohua Zheng
Summary: Physical exercise interventions have a positive effect on working memory, cognitive flexibility, and inhibitory control in cognitively healthy adults aged 60 and above. Aerobic exercise lasting over 13 weeks, mind-body exercise, and interventions lasting over 26 weeks show significant improvements in executive function.
INTERNATIONAL JOURNAL OF NURSING STUDIES
(2021)
Article
Food Science & Technology
Yingying Zheng, Long Tang, Mingguang Yu, Ting Li, Huanlu Song, Pei Li, Ku Li, Jian Xiong
Summary: Research should focus on developing novel agents to replace salt in foods without affecting taste, to avoid health risks associated with high-salt diets. Some yeast extracts can be used as salt substitutes without imparting additional odors. Salty peptides were fractionated from Angel Yeast in this study.
JOURNAL OF FOOD SCIENCE AND TECHNOLOGY-MYSORE
(2021)
Article
Computer Science, Information Systems
Xianzhong Long, Jian Xiong, Lei Chen
Summary: The new method RAGDNMF combines robustness, adaptive graph learning and discrimination information, aiming to learn a good projection matrix for removing redundant information while preserving effective components. Face recognition experiments on four benchmark datasets demonstrate the effectiveness of the proposed method.
MULTIMEDIA TOOLS AND APPLICATIONS
(2021)
Article
Computer Science, Hardware & Architecture
Jian Xiong, Xinzhong Zhu, Jie Yuan, Ran Shi, Hao Gao
Summary: This paper proposes a perceptual visual security assessment metric by fusing local and global feature similarity, which combines the distortion of structural information, leakage of important visual information, and changes in frequency components. Experimental results show that the proposed metric achieves significantly higher performance and robustness than existing metrics.
COMPUTERS & ELECTRICAL ENGINEERING
(2021)
Review
Integrative & Complementary Medicine
Jian Xiong, WenChuan Qi, Han Yang, SiTing Zou, Jing Kong, ChengLong Wang, YuanFang Zhou, FanRong Liang
Summary: This study systematically evaluated the clinical efficacy and safety of acupuncture in treating cough-variant asthma, showing that acupuncture intervention can enhance the total clinical effectiveness rate, reduce relapse rate, relieve symptoms, and improve related indicators. However, more high-quality clinical randomized controlled trials are needed to further verify the efficacy and safety of this treatment.
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2021)
Article
Biochemistry & Molecular Biology
Jin-Qiong Zhan, Chun-Nuan Chen, Si-Xian Wu, Han-Jun Wu, Ke Zou, Jian-Wen Xiong, Bo Wei, Yuan-Jian Yang
Summary: The study shows that fisetin treatment can reverse deficits in hippocampal synaptic plasticity and memory in a male rat model of schizophrenia by restoring the phosphorylation and surface expression of AMPAR GluA1 subunit, indicating fisetin as a promising therapeutic candidate for schizophrenia-associated cognitive deficits.
JOURNAL OF NEUROCHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Xiaodan Li, Jian Xiong, Baojian Zhang, Dongting Zhangsun, Sulan Luo
Summary: Morphine, a common analgesic, has limited clinical application due to abuse potential. Nicotinic acetylcholine receptors (nAChRs) in the brain play a key role in drug addiction. The study discovered a selective ligand, alpha-Conotoxin TxIB, which inhibits a specific type of nAChRs and may be useful in mitigating drug addiction.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Integrative & Complementary Medicine
Wenchuan Qi, Xiang Li, Yanrong Ren, Xueying Liu, Hongjuan Fu, Xiao Wang, Xiao Li, Jian Xiong, Qianhua Zheng, Dingjun Cai, Fanrong Liang
Summary: The study revealed that electroacupuncture at the PC6 point can inhibit the process of myocardial fibrosis by reducing the expression of IncRNA Miat, suggesting it as a potential therapeutic method for myocardial fibrosis.
Article
Integrative & Complementary Medicine
Jian Xiong, Ziwen Wang, Minmin Ruan, Hengshan Yao, Miao Wei, Ruirui Sun, Xuejie Yang, Wenchuan Qi, Fanrong Liang
Summary: Neuroimaging studies on the effects of acupuncture have been conducted since the 1960s, with China, the United States, and South Korea leading in research. The focus of current research is on pain and neurofunctional rehabilitation.
COMPLEMENTARY THERAPIES IN MEDICINE
(2022)
Review
Clinical Neurology
Fayang Ling, Wenchuan Qi, Xiao Li, Jun Zhou, Jian Xiong, Yi Zhao, Qianhua Zheng, Fanrong Liang
Summary: Cancer pain is a common symptom that greatly affects the quality of life for cancer patients. Acupuncture has been found to have curative effects on cancer pain. This study aims to analyze and visualize the current status and research trends of acupuncture treatment for cancer pain over the past decade and provide directions for future development.
JOURNAL OF PAIN RESEARCH
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Jian Xiong, Xiang Li, Hongjuan Fu, Xinye Luo, Xiao Li, Yanrong Ren, Xueying Liu, Qianhua Zheng, Wenchuan Qi, Fanrong Liang
Summary: Infrared thermal imaging technology was used to observe the changes in infrared radiation temperature at acupoints in rats with chronic myocardial ischemia injury. The study found that myocardial ischemic injury can cause a decrease in the IR temperature on the body surface of bilateral Neiguan (PC6) acupoints, suggesting that visceral diseases can affect the energy metabolism of acupoints.
CURRENT MEDICAL IMAGING
(2023)
Article
Energy & Fuels
Jiangwei Shen, Jian Xiong, Xing Shu, Guang Li, Yuanjian Zhang, Zheng Chen, Yonggang Liu
Summary: This paper proposes an advanced framework to estimate SOC for lithium-ion batteries considering temperature variation. By establishing an accurate electrical model and optimizing model parameters with genetic algorithm, combined with Kalman filter algorithm, it can accurately evaluate battery SOC under complex temperature environments.
INTERNATIONAL JOURNAL OF ENERGY RESEARCH
(2021)
Review
Geriatrics & Gerontology
Mingzhu Ye, Lecong Wang, Jian Xiong, Guohua Zheng
Summary: Mind-body exercise has a positive impact on memory in older adults, showing improvements in general memory, short-term memory, long-term memory, working memory, episodic memory, and semantic memory. Compared to no specific exercise intervention, mind-body exercise enhances memory in older adults.
AGING CLINICAL AND EXPERIMENTAL RESEARCH
(2021)
Article
Chemistry, Organic
Fuying Zhu, Yamei Lin
Summary: In this study, a low-metal iron-supported catalyst (Fe20/NC-Mg) was reported for the efficient synthesis of quinoxaline compounds, using water as a solvent and without additional bases. The synergistic effect of FeNx site and Mg (OH)2 nanorods in the catalyst played a key role in achieving high yields (82-91%) in 16 examples. The gram-level synthesis and reusability of the catalysts after four cycles demonstrated its industrial application potential.
Article
Chemistry, Organic
Mikhail Kozlov, Alexey Tyurin, Andrey Dmitrenok, Vyacheslav Rusak, Aleksander Fedorov, Igor Zavarzin, Yulia Volkova
Summary: This study presents a novel and practical synthesis method for phosphorus-substituted 1,3,4-thiadiazolines using phosphorylthioformic acid hydrazides and ketones. The protocol demonstrates operational simplicity, availability of reagents, and tolerance towards different functional groups.
Article
Chemistry, Organic
Jisna Jose, Thomas Mathew
Summary: 2-Cyclopentenone and its derivatives are highly esteemed synthetic intermediates with exceptional utility in organic synthesis. They are favored structural motifs in numerous pharmaceutical drugs and natural products, highlighting their significance. The review discusses the various methods used to synthesize cyclopentenones from 2016 to 2023.
