Highly efficient synthesis of DNA-binding hairpin polyamides via the use of a new triphosgene coupling strategy.

作者: Wu Su , Stephen J. Gray , Ruggero Dondi , Glenn A. Burley

DOI: 10.1021/OL9015139

关键词:

摘要: A facile and highly efficient solid phase synthesis method is reported for the preparation of hairpin DNA-binding polyamides using cost-effective triphosgene (BTC) activating agent. Difficult polyamide sequences were prepared from N-methylimidazole (Im) N-methylpyrrole (Py) building blocks with high stepwise yields (>98%) Boc chemistry. The versatility coupling approach was also demonstrated first time on aryl hydrazine resins to afford biomedically relevant tail-truncated in excellent isolated yields.

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