329187-59-9Relevant articles and documents
Preparation method of 4-[(4,6-dichloro-2-pyrimidinyl)amino]cyanophenyl
-
Paragraph 0023-0028, (2019/11/14)
The invention provides a method for synthesizing 4-[(4,6-dichloro-2-pyrimidinyl)amino]cyanophenyl (III). The method comprises the steps that 2-amino-4,6-dichloropyrimidine (II) is taken as a raw material to be mixed with 4-fluorobenzonitrile (I) in the presence of sodium hydride, and a one-step method is adopted for synthesis. The method for synthesizing the 4-[(4,6-dichloro-2-pyrimidinyl)amino]cyanophenyl (III) has the advantages that the operation is simple, the purity and yield of the product are higher, and industrialized practical significance and social and economic benefits are provided.
Process for the Synthesis of Etravirine and Its Intermediates
-
Paragraph 0031; 0032, (2015/12/05)
The invention discloses the synthesis of Etravirine via intermediate 4-((4-amino-5-bromo-6-chloropyrimidin-2-yl) amino)benzonitrile and process for the preparation of Etravirine of the formula-I.
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility
Bollini, Mariela,Cisneros, José A.,Spasov, Krasimir A.,Anderson, Karen S.,Jorgensen, William L.
, p. 5213 - 5216 (2013/09/12)
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the entrance channel of the NNRTI binding site. Compound 4d shows low-nanomolar activity similar to etravirine towards wild-type HIV-1 and key viral variants.