15768-07-7Relevant articles and documents
Efficient and recyclable solid acid-catalyzed alkylation of active methylene compound via oxonium intermediate for atom economical synthesis of organic compounds
Naikwadi, Dhanaji R.,Bankar, Balasaheb D.,Ravi, Krishnan,Biradar, Ankush V.
, p. 3691 - 3703 (2021/06/12)
In the present work, we report the catalytic reaction of active methylene compounds with cyclic enol ethers and aryl acetals through oxonium intermediate under solvent-free conditions using heterogeneous solid acid catalysts. Among studied solid acid catalysts, Amberlyst-15 gave excellent yields (35–85%) of alkylated products. The catalyst showed broader substrate scope, and a recyclable catalytic cost-efficient approach of the alkylation was examined on the different types of cyclic enol ethers and aryl acetal.
Cross-linked polystyrene-TiCl4 complex as a reusable Lewis acid catalyst for solvent-free Knoevenagel condensations of 1,3-dicarbonyl compounds with aldehydes
Rahmatpour, Ali,Goodarzi, Niloofar
, p. 24 - 31 (2019/03/08)
Cross-linked polystyrene copolymer beads with the average particle size in the range of (50–80 mesh size) were prepared by a new method, characterized and functionalized with titanium tetrachloride to afford the corresponding polystyrene?titanium tetrachloride complex in one step reaction and characterized by FT-IR, UV, TGA, DSC, XRD, SEM, BET. This polymer metal complex (PS/TiCl4) was used as a heterogeneous, recoverable, reusable Lewis acid for solvent-free Knoevenagel condensations of 1,3-diketones with aromatic aldehydes under green and mild conditions. The rate of reactions was found to decrease with an increasing percentage of crosslinking and the mesh size of the copolymer beads. This complex showed good stability and catalytic activity in the Knoevenagel reactions.
Design and synthesis of orally bioavailable 4-methyl heteroaryldihydropyrimidine based hepatitis B virus (HBV) capsid inhibitors
Qiu, Zongxing,Lin, Xianfeng,Zhou, Mingwei,Liu, Yongfu,Zhu, Wei,Chen, Wenming,Zhang, Weixing,Guo, Lei,Liu, Haixia,Wu, Guolong,Huang, Mengwei,Jiang, Min,Xu, Zhiheng,Zhou, Zheng,Qin, Ning,Ren, Shuang,Qiu, Hongxia,Zhong, Sheng,Zhang, Yuxia,Zhang, Yi,Wu, Xiaoyue,Shi, Liping,Shen, Fang,Mao, Yi,Zhou, Xue,Yang, Wengang,Wu, Jim Z.,Yang, Guang,Mayweg, Alexander V.,Shen, Hong C.,Tang, Guozhi
, p. 7651 - 7666 (2016/09/04)
Targeting the capsid protein of hepatitis B virus (HBV) and thus interrupting normal capsid formation have been an attractive approach to block the replication of HBV viruses. We carried out multidimensional structural optimizations based on the heteroaryldihydropyrimidine (HAP) analogue Bay41-4109 (1) and identified a novel series of HBV capsid inhibitors that demonstrated promising cellular selectivity indexes, metabolic stabilities, and in vitro safety profiles. Herein we disclose the design, synthesis, structureactivity relationship (SAR), cocrystal structure in complex with HBV capsid proteins and in vivo pharmacological study of the 4-methyl HAP analogues. In particular, the (2S,4S)-4,4-difluoroproline substituted analogue 34a demonstrated high oral bioavailability and liver exposure and achieved over 2 log viral load reduction in a hydrodynamic injected (HDI) HBV mouse model.
