The Use of Glycidyl Ethers Involving Aziridinium Intermediates and Other Methodology for the Preparation of Enantiomerically Pure Drug Candidates

…, TJN Watson, W Subotkowski, J Daniel…

文献索引：Ayers, Timothy A.; Watson, Timothy J. N.; Subotkowski, Witold; Daniel, John; Webster, Mark Organic Process Research and Development, 2012 , vol. 16, # 1 p. 141 - 147

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被引用次数: 2

摘要

An enantiospecific 1, 2-amine migration process through an aziridinium intermediate involving ring-opening with potassium phthalimide derivatives to produce precursors to drug candidates was developed. The precursor amine derivatives were readily available by epoxide opening of simple glycidyl ether derivatives. The regioselectivity of the process was shown to provide approximately 85% of the desired rearranged product with subsequent ...