- H2-Acceptorless Dehydrogenative Boration and Transfer Boration of Alkenes Enabled by Zirconium Catalyst
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The first example of an efficient and direct dehydrogenative boration of alkenes for vinyl boronate ester synthesis was achieved using a zirconium catalyst. Our methodology avoids using precious transition metals, additional hydrogen acceptors, high temperatures, and long reaction times, which were required to overcome the reducing ability of borane, to give alkyl boronate esters. Detailed mechanistic studies revealed a reversible reaction pathway and further suggested applying the zirconium complex as a “shuttle catalyst” for transfer boration, which thus sidesteps the use of relatively sensitive borane.
- Shi, Xiaonan,Li, Sida,Wu, Lipeng
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Read Online
- Design, synthesis, and biological evaluation of novel 2′-methyl-2′-fluoro-6-methyl-7-alkynyl-7-deazapurine nucleoside analogs as anti-Zika virus agents
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Zika virus (ZIKV) is a mosquito-borne flavivirus and outbreaks of ZIKV have been reported in Africa, Americas and other parts of the world lately. The ZIKV epidemic has received extensive attention due to its ability to cause serious medical consequences and complications such as microcephaly and Guillain-Barre syndrome in recent years. Up to now, there are no specific treatments or vaccines available for ZIKV infection, which highlights the urgent need for developing new therapies. In this work, we designed and synthesized a series of novel 6-methyl-7-acetylenenyl-7-deazapurine nucleoside analogs as potential inhibitors of ZIKV replication. The biological activities against ZIKV replication were evaluated and the structure-activity relationship (SAR) was also studied. Among the compounds evaluated, nucleoside analog 38 (EC50 = 2.8 ± 0.8 μM, EC90 = 6.8 ± 2.3 μM) showed the most potent anti-ZIKV activity with low cytotoxicity (CC50 = 54.1 ± 6.9 μM) in an A549 based cellular model. The inhibitory activity of 38 was about 5 times more potent than the positive control NITD008. Notably, 38 showed similar inhibition potency against different ZIKV strains (ZG-01 and MR766) in a variety of host cell types including SNB19, A549, Huh7, Vero. In addition, 38 (Kd = 1.87 μM) has a stronger affinity to ZIKV RNA-dependent RNA polymerase (RdRp) protein than NITD008 (Kd = 3.43 μM) in the non-phosphorylation assay. These results indicated that compound 38 may serve as a promising candidate in future anti-ZIKV drug discovery.
- Yao, Guoqiang,Yu, Jianchen,Lin, Cai,Zhu, Yujia,Duan, Anna,Li, Mengfeng,Yuan, Jie,Zhang, Jiancun
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supporting information
(2022/03/23)
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- Electrochemically promoted decarboxylative borylation of alkyl N-hydroxyphthalimide esters
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An electrochemically promoted decarboxylative borylation reaction is reported. The reaction proceeds under mild conditions in an undivided cell without use of transition metal- or photo-catalysts. The key feature of the reaction is the compatibility of di
- Dai, Jian-Jun,Fang, Wen,Teng, Xin-Xin,Xu, Hua-Jian,Xu, Jun
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- Method for rapidly preparing cyclopropane derivative based on microchannel reaction technology
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The invention discloses a method for rapidly preparing a cyclopropane derivative based on a microchannel reaction technology, which comprises an alkaline hydrolysis reaction and an electrophilic addition reaction. The alkaline hydrolysis reaction comprise
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Paragraph 0050-0052
(2021/08/06)
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- Enantioselective synthesis of trans-aryl-and-heteroaryl-substituted cyclopropylboronates by copper (I)-catalyzed reactions of allylic phosphates with a diboron derivative
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A new asymmetric route for the synthesis of trans-2-aryl- and -heteroaryl-substituted cyclopropylboronates has been developed. (Z)-3-arylallylic phosphates were converted to the optically active products with high yield and diastereo- and enantioselectivity through a copper(I)-catalyzed reaction with a diboron derivative. Under mild reaction conditions, the reaction affords the arylcyclopropane products with a functional group and a heteroaromatic group in a highly enantioselective manner. When (E)-allylic phosphates were used as substrates, a ligand-controlled product switch between the trans and cis configurations was observed.
- Zhong, Chongmin,Kunii, Shun,Kosaka, Yuki,Sawamura, Masaya,Ito, Hajime
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p. 11440 - 11442
(2010/10/04)
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- MANUFACTURING METHOD OF ORGANOBORON COMPOUND
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A manufacturing method for one of, or a mixture of, an optically active allylboron compound and racemic or optically active boryl cyclopropane, including a coupling reaction, in the presence of a catalyst, between allyl compound and diboron compound. It i
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Page/Page column 12
(2008/12/04)
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- INDOLES USEFUL IN THE TREATMENT OF INFLAMMATION
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There is provided compounds of formula (I), Wherein X1 , R1 , R2 , R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.
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Page/Page column 122
(2008/06/13)
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