Kuyl-Yeheskiely E, Tromp C M, Schaeffer A H, van der Marel G A, van Boom J H
Nucleic Acids Res. 1987 Feb 25;15(4):1807-18. doi: 10.1093/nar/15.4.1807.
The monofunctional phosphitylating reagents bis-(N,N-diethylamino)chlorophosphine and salicylchlorophosphine have been applied for the preparation of H-phosphonates of the amino acids serine, threonine and tyrosine. Experimental evidence showed that the latter reagent was less effective for the synthesis of a tyrosine H-phosphonate. The amino acids (peptide) H-phosphonates of serine or threonine proved to be suitable starting compounds for the formation of a phosphate diester bond with the 5'-OH of a d-nucleoside derivative using pivaloyl chloride as the activating reagent.
单功能磷酰化试剂双（N，N - 二乙氨基）氯膦和水杨酰氯膦已用于制备氨基酸丝氨酸、苏氨酸和酪氨酸的H-膦酸酯。实验证据表明，后一种试剂在合成酪氨酸H-膦酸酯方面效果较差。事实证明，丝氨酸或苏氨酸的氨基酸（肽）H-膦酸酯是使用新戊酰氯作为活化试剂与d-核苷衍生物的5'-OH形成磷酸二酯键的合适起始化合物。
