The facile preparation of primary and secondary amines via an improved Fukuyama-Mitsunobu procedure. Application to the synthesis of a lung-targeted gene delivery agent |
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Authors: | Guisado Cristina Waterhouse Jodie E Price Wayne S Jorgensen Michael R Miller Andrew D |
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Institution: | IC-Vec Ltd., Flowers Building, Armstrong Road, London SW7 2AZ, UK. |
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Abstract: | An efficient modification of the Fukuyama-Mitsunobu procedure has been developed whereby primary or secondary amines can be synthesized from alkyl alcohols and the corresponding nosyl-protected/activated amine. Most importantly, the use of the DTBAD and diphenylpyridinylphosphine, as Mitsunobu reagents, generates reaction by-products that can be easily removed, providing a remarkably clean product mixture. This improved technique was implemented in the synthesis of a complex lipopeptide designed to target alpha9beta1-integrin proteins predominant on upper airway epithelial cells. |
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