31603-77-7Relevant articles and documents
Rapid and Simple Access to α-(Hetero)arylacetonitriles from Gem-Difluoroalkenes
Hu, Dandan,Liu, Jiayue,Ren, Hongjun,Song, Jinyu,Zhang, Jun-Qi,Zhu, Guorong
supporting information, p. 786 - 790 (2022/01/28)
A scalable cyanation of gem-difluoroalkenes to (hetero)arylacetonitrile derivatives was developed. This strategy features mild reaction conditions, excellent yields, wide substrate scope, and broad functional group tolerance. Significantly, in this reacti
Biphenyl acetic acid and preparation method thereof
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, (2020/09/09)
The invention discloses biphenyl acetic acid and a preparation method thereof. The preparation method comprises the following steps: dissolving bromobenzene into dimethylformamide, and performing reaction under the action of palladium powder to obtain biphenyl; dissolving biphenyl in cyclohexane, and performing chloromethylation reaction on biphenyl in a hydrochloric acid solution and a saturatedformaldehyde aqueous solution to obtain an intermediate 1; dissolving sodium cyanide in deionized water, and performing cyanidation reaction on the intermediate 1 and a sodium cyanide aqueous solutionunder the action of a catalyst n-butylammonium bromide to obtain an intermediate 2; and further hydrolyzing the intermediate 2 under the condition of an alkaline aqueous solution, and performing acidifying under the action of hydrochloric acid to obtain biphenyl acetic acid. The yield of the biphenyl acetic acid prepared by the aid of the method is higher than that of the biphenyl acetic acid prepared by the aid of traditional processes, reactants are low in price, the preparation cost of the biphenyl acetic acid can be greatly reduced, and the method is favorable for market popularization.
Design of biphenyl-substituted diarylpyrimidines with a cyanomethyl linker as HIV-1 NNRTIs via a molecular hybridization strategy
Chen, Fen-Er,Han, Sheng,Lei, Yuan,Pannecouque, Christophe,Yang, Yang,Zhuang, Chunlin,de Clercq, Erik
, (2020/03/17)
The key problems of human immunodeficiency virus (HIV) therapy are the rapid emergence of drug-resistant mutant strains and significant cumulative drug toxicities. Therefore, there is an urgent demand for new anti-HIV agents with low toxicity and broad-spectrum antiviral potency. A series of biphenyl-substituted diarylpyrimidines with a cyanomethyl linker were designed using a molecular hybridization strategy. The cell-based anti-HIV assay showed that most of the compounds exhibited moderate to good activities against wild-type HIV-1 and clinically relevant mutant strains with a more favorable toxicity, and the enzymatic assay showed they had nanomolar activity against reverse transcriptase (RT). Compound 10p exhibited the best activity against wild-type HIV-1 with an EC50 (50% HIV-1 replication inhibitory concentration) value of 0.027 μM, an acceptable CC50 (50% cytotoxic concentration) value of 36.4 μM, and selectivity index of 1361, with moderate activities against the single mutants (EC50: E138K, 0.17 μM; Y181C, 0.87 μM; K103N, 0.9 μM; L100I, 1.21 μM, respectively), and an IC50 value of 0.059 μM against the RT enzyme, which was six-fold higher than nevirapine (NVP). The preliminary structure–activity relationship (SAR) of these new compounds was concluded. The molecular modeling predicted the binding modes of the new compounds with RT, providing molecular insight for further drug design.
