- Substituted 1-methyl-4-phenylpyrrolidin-2-ones – Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors
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N-Methylpyrrolidone is one of several chemotypes that have been described as a mimetic of acetyl-lysine in the development of bromodomain inhibitors. In this paper, we describe the synthesis of a 4-phenyl substituted analogue – 1-methyl-4-phenylpyrrolidin-2-one – and the use of aryl substitution reactions as a divergent route for derivatives. Ultimately, this has led to structurally complex, chiral compounds with progressively improved affinity as inhibitors of bromodomain-containing protein 4.
- Hilton-Proctor, J. P.,Ilyichova, O.,Jennings, I. G.,Johnstone, R. W.,Mountford, S. J.,Scanlon, M. J.,Shortt, J.,Thompson, P. E.,Zheng, Z.
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- Method for synthesizing 4-amino-3-phenylbutyric acid hydrochloride
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The invention provides a method for synthesizing 4-amino-3-phenylbutyric acid hydrochloride. The synthetic method comprises the following steps: preparing methyl 4-nitro-3-phenyl butyrate, preparing methyl 4-amino-3-phenyl butyrate, and treating to obtain the product. According to the synthetic method disclosed by the invention, a complete process for synthesizing 4-amino-3-phenylbutyric acid hydrochloride is created, the synthetic method is simple in process, high in yield and low in cost, and the main problems that the initial raw materials used in the conventional process are high in price, the operation steps are onerous and pollution in the production process is severe are solved.
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