Debaene François, Winssinger Nicolas
Institut de Science et Ingénierie Supramoleculaires, Université Louis Pasteur, 8 allée Gaspard Monge, 67000 Strasbourg, France.
Org Lett. 2003 Nov 13;5(23):4445-7. doi: 10.1021/ol0358408.
[reaction: see text] A practical and efficient method for PNA synthesis using an azide group to mask the N-terminus is reported. The deprotection was carried out in 5 min, while couplings were complete within 60 min. The near neutral conditions of the phosphine deprotection combined with the base-free coupling using hydroxybenzotriazole-activated monomers make this approach very mild.
[反应:见正文] 报道了一种使用叠氮基团掩蔽N端进行肽核酸(PNA)合成的实用且高效的方法。脱保护在5分钟内完成,而偶联反应在60分钟内完成。膦脱保护的近中性条件与使用羟基苯并三唑活化单体的无碱偶联相结合,使得该方法非常温和。