Shaw Arthur Y, Medda Federico, Hulme Christopher
Department of Pharmacology and Toxicology, College of Pharmacy, BIO5 Oro Valley, 1580 E. Hanley Blvd, The University of Arizona, Tucson, AZ.
Tetrahedron Lett. 2012 Mar 14;53(11):1313-1315. doi: 10.1016/j.tetlet.2011.12.073.
The following report describes novel methodology for the rapid synthesis of unique conformationally constrained norstatine analogs of potential biological relevance. A PADAM (Passerini reaction - Amine Deprotection - Acyl Migration reaction) sequence is followed by a TFA-mediated microwave-assisted cyclization to generate the final benzimidazole isostere of the norstatine scaffold in moderate to good yields. The applicability of this solution phase methodology to the preparation of a small collection of compounds is discussed.
以下报告描述了用于快速合成具有潜在生物学相关性的独特构象受限去甲他汀类似物的新方法。先进行PADAM（帕瑟里尼反应 - 胺脱保护 - 酰基迁移反应）序列，然后进行三氟乙酸介导的微波辅助环化反应，以中等至良好的产率生成去甲他汀骨架的最终苯并咪唑电子等排体。讨论了这种溶液相方法在制备一小批化合物中的适用性。
