2-氨基苯并噻唑的固相合成。
Solid phase synthesis of 2-aminobenzothiazoles.
机构信息
Department of Chemistry, University of Pennsylvania, 231 South 34th St., Philadelphia, PA 19104-6323, United States.
出版信息
Bioorg Med Chem Lett. 2010 Jan 15;20(2):644-8. doi: 10.1016/j.bmcl.2009.11.055. Epub 2009 Dec 1.
Abstract
A traceless solid supported protocol for the synthesis of 2-aminobenzothiazoles is described, employing resin-bound acyl-isothiocyanate and a series of anilines. Cyclization of the resulting N-acyl, N'-phenyl-thioureas generates the 2-aminobenzothiazole scaffold, which can be further elaborated prior to hydrazine-mediated cleavage of the final products from the carboxy-polystyrene resin. A small, focused library of 2-aminobenzothiazoles was prepared.
摘要
描述了一种无痕固相支撑法合成 2-氨基苯并噻唑的方法，采用树脂结合的酰基异硫氰酸酯和一系列苯胺。所得 N-酰基、N'-苯基-硫脲的环化生成 2-氨基苯并噻唑骨架，然后可以在肼介导的从羧基聚苯乙烯树脂上裂解最终产物之前对其进行进一步修饰。合成了一个小的、重点关注的 2-氨基苯并噻唑文库。
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