A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists |
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| Authors: | Zhu Yun-Fei Wilcoxen Keith Saunders John Guo Zhiqiang Gao Yinghong Connors Patrick J Gross Timothy D Tucci Fabio C Struthers R Scott Reinhart Greg J Xie Qiu Chen Chen |
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| Affiliation: | Neurocrine Biosciences, Inc., 10555 Science Center Drive, San Diego, CA 92121, USA. fzhu@neurocine.com |
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| Abstract: | In the process of developing GnRH receptor antagonists, a novel base-catalyzed cyclization of compounds 5a-b was discovered, which led to the formation of the 2-aryl pyrrolo[1,2-a]pyrimid-7-one core structures 6a-b. These intermediates were further modified at positions 1, 2, 4 and 6 to afford a series of potent GnRH antagonists with low nanomolar K(i) values. |
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