Convenient and Efficient“One-pot”Synthesis of N-(1,3-Diphenyl-1H-pyrazole-5-yl)amide Derivatives: Positive allosteric Modulators of mGluR5

• Main Authors: Wei-Nien Su, 蘇威年
• Other Authors: 翁豐富
• Format: Others
• Language: zh-TW
• Published: 2008
• Online Access: http://ndltd.ncl.edu.tw/handle/14099096043064355484

碩士 === 中國醫藥大學 === 藥物化學研究所 === 96 === Glutamate is the major excitatory transmitter in the mammalian central nervous system. Metabotropic glutamate receptors (mGluRs) play an important role in controlling neuronal excitability and synaptic transmission in the central nervous system (CNS) of the mammalian brain. N-(1.3-Diphenylare1-H-pyrazol-5-yl)benzamide derivatives were recently developed as the first centrally active positive allosteric modulator of rat and human metabotropic glutamate receptor mGluR5 subtype. N-(1,3- diphenyl-1H-pyrazol-5-yl)amide derivatives were convenient and efficient synthesized by using phenylhydrazine, benzoylacetonitrile, and a series of acylation agents. Two steps of condensation-cyclization and acylation were performed in one-pot to give the corresponding N-(1,3-diphenyl-1H-pyrazol-5-yl)amide analogues in good to excellent yields (70–90%).