共查询到20条相似文献,搜索用时 15 毫秒
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Solid-phase organic synthesis is a rapidly expanding area of synthetic chemistry that is being widely exploited in the search for new medicinally important compounds using combinatorial techniques. In recent decades, a large number of reports related to solid-phase synthesis of heterocycles have appeared because of the wide variety of their biological activity. In this review, we report the important role of solid-phase synthesis in the synthesis of nitrogen containing six-membered ring heterocycles. 相似文献
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In recent decades, a large number of reports related to solid-phase synthesis of heterocycles have appeared, owing to the wide variety of their biological activity. This review introduces the key concepts of solid-phase methodology and combinatorial synthesis with particular focus on the important role of solid-phase synthesis in the synthesis of nitrogen-containing five-membered ring heterocycles. 相似文献
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Changtong Zhu Zhenbo Yuan Zhiwei Deng Dejing Yin Yan Zhang Jingwen Zhou Yijian Rao 《Angewandte Chemie (International ed. in English)》2023,62(50):e202311762
New-to-nature biocatalysis in organic synthesis has recently emerged as a green and powerful strategy for the preparation of valuable chiral products, among which chiral oxygen-containing benzo-fused heterocycles are important structural motifs in pharmaceutical industry. However, the asymmetric synthesis of these compounds through radical-mediated methods is challenging. Herein, a novel asymmetric radical-mediated photoenzymatic synthesis strategy is developed to realize the efficient enantioselective synthesis of oxygen-containing benzo-fused heterocycles through structure-guided engineering of a flavin-dependent ‘ene’-reductase GluER. It shows that variant GluER-W100H could efficiently produce various benzoxepinones, chromanone and indanone with different benzo-fused rings in high yields with great stereoselectivities under visible light. Moreover, these results are well supported by mechanistic experiments, revealing that this photoenzymatic process involves electron donor-acceptor complex formation, single electron transfer and hydrogen atom transfer. Therefore, we provide an alternative green approach for efficient chemoenzymatic synthesis of important chiral skeletons of bioactive pharmaceuticals. 相似文献
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Josef Stadlwieser Ernst P. Ellmerer-Müller Andreas Tak Najib Maslouh Willi Bannwarth 《Angewandte Chemie (International ed. in English)》1998,37(10):1402-1404
A nine-step (!) solid-phase synthesis and subsequent cleavage with cyclization from the polymeric support were the keys to preparing high-quality molecular libraries of thiazolylhydantoines 1 from modified amino acid building blocks. Each step in the synthesis is different. Because the final cyclization cleaves only molecules that have been successfully constructed, the products obtained are pure. R1, R2=alkyl; R3=aryl, arylO; R4=allyl. 相似文献
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Dr. Markus Julian Schöwe Dr. Odin Keiper Prof. Dr. Carlo Unverzagt Prof. Dr. Valentin Wittmann 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(69):15759-15764
A general and robust method for the incorporation of aspartates with a thioacid side chain into peptides has been developed. Pseudoproline tripeptides served as building blocks for the efficient fluorenylmethyloxycarbonyl (Fmoc) solid-phase synthesis of thioacid-containing peptides. These peptides were readily converted to complex N-glycopeptides by using a fast and chemoselective one-pot deprotection/ligation procedure. Furthermore, a novel side reaction that can lead to site-selective peptide cleavage using thioacids (CUT) was discovered and studied in detail. 相似文献
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Navjeet Kaur 《合成通讯》2013,43(4):403-431
The development of new strategies for the synthesis of small-sized heterocycles has remained a highly attractive but challenging proposition. An overview of the application of microwave irradiation in three nitrogen atoms containing fused five-membered heterocyclic compounds synthesis is presented, focusing on the developments in the past 5–10 years. This contribution covers the literature concerning the total synthesis of N,N,N-heterocycles. The literature data are summarized based on the type of cycles. 相似文献
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A new method upon adopting a solid-phase strategy for synthesis of N-aryl succinimides is described here, using the silica-bound benzoyl chloride (SBBC) as dehydrating agent in reaction with N-arylsuccinamic acids. The main advantage of this method is the recyclability of SBBC. 相似文献
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Solid-Phase Synthesis of Calcium Carbide in a Plasma Reactor 总被引:1,自引:0,他引:1
A laboratory-scale spout-fluid bed reactor with a dc plasma torch was used to study the solid-phase synthesis of calcium carbide. Calcium oxide powder with a mean particle size of 170 m was reacted with graphite powder (130 m). Argon was used to initiate the plasma and hydrogen gas was then added to increase power and raise the plasma jet enthalpy. Experimental results showed that the reaction took place in the vicinity of the plasma jet and that conversion to calcium carbide increased linearly with reaction time. The rate of conversion increased exponentially with plasma jet temperature, indicating that chemical reaction was the controlling mechanism. Microscopic analysis of the solid product showed that calcium carbide was formed around both reactants, and that the reaction followed a shrinking core model. Although melting and agglomeration of partially reacted particles occurred at high temperature, resulting in instability of the bed and impeding the reaction progress, high conversions are expected in a continuous process with optimized reactor design. 相似文献
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The development of new strategies for synthesis of six-membered O-heterocycles has remained a highly attractive but challenging proposition. An overview of the application of microwave irradiation in oxygen-containing six-membered heterocyclic compounds synthesis is presented, focusing on the developments in the past 5–10 years. This contribution covers the literature concerning the total synthesis of six membered O-heterocycles. 相似文献
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Navjeet Kaur 《合成通讯》2014,44(24):3483-3508
The development of new strategies for synthesis of five-membered O-heterocycles has remained a highly attractive but challenging proposition. An overview of the application of microwave irradiation in oxygen-containing five-membered heterocyclic compound synthesis is presented, focusing on the developments in the past 5–10 years. This contribution covers the literature concerning the total synthesis of five-membered O-heterocycles. 相似文献
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The development of new strategies for synthesis of medium-sized O-heterocycles has remained a highly attractive but challenging proposition. An overview of the application of microwave irradiation in oxygen-containing seven- and higher-membered heterocyclic compounds synthesis is presented, focusing on the developments in the past 5–10 years. This contribution covers the literature concerning the total synthesis of O-heterocycles. The literature data are summarized based on the size of cycles. 相似文献
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The development of new strategies for synthesis of six-membered O,O-heterocycles has remained a highly attractive but challenging proposition. An overview of the application of microwave irradiation in two oxygen atoms containing six-membered heterocyclic compounds synthesis is presented, focusing on the developments in the past 5–10 years. This contribution covers the literature concerning the total synthesis of six-membered O,O-heterocycles. 相似文献
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The cellular plasma membrane plays a fundamental role in biological processes, including cell growth, signaling and transport. The labelling of the plasma membrane with targeted fluorescent probes offers a convenient and non-invasive way to image the morphological changes and dynamics of a membrane in real-time and, despite many examples of fluorescent plasma membrane probes, a “universal targeting/anchoring moiety” is still required. In this study, a small number of stearic acid-based probes labelled with 6-carboxyfluorescein was designed and fabricated via solid-phase synthesis in which variations in both charge and hydrophobicity were explored. To ease the synthesis process, a gram-scale synthesis of the Fmoc-Lys(6-carboxyfluoresein diacetate)-OH building block was developed, allowing the discovery of optimal probes that carried a positively charged amino group and a stearic acid tail that exhibited intense plasma membrane brightness and robust retention. 相似文献