Hayakawa Y, Kawai R, Kataoka M
Laboratory of Bioorganic Chemistry, Graduate School of Human Informatics, Nagoya University, Chikusa, 464-8601, Nagoya, Japan.
Eur J Pharm Sci. 2001 Apr;13(1):5-16. doi: 10.1016/s0928-0987(00)00202-5.
Oligonucleotide synthesis via methods without nucleobase protection (N-unprotected methods) is briefly reviewed. The N-unprotected methods are advantageous in the following respects over conventional approaches that use protectors, generally, acyl protectors for the nucleobase (N-protected method). Two steps, introduction and removal of the protecting groups, are eliminated, and consequently use of undesirable reagents involved in these steps are avoided. In the synthesis of DNA oligomers, the risk of depurination of deoxyadenosine and deoxyguanosine derivatives, which is a serious problem in the N-protected methods, is considerably reduced. The range of synthesizable artificial analogues bearing base-labile functions is extended because harsh base treatment for the deprotection is eliminated.
简要回顾了通过无碱基保护方法（N-无保护方法）进行的寡核苷酸合成。与使用保护基（通常是用于碱基的酰基保护基）的传统方法（N-保护方法）相比，N-无保护方法在以下方面具有优势。省去了引入和去除保护基这两个步骤，因此避免了这些步骤中所涉及的不良试剂的使用。在DNA寡聚体的合成中，N-保护方法中严重存在的脱氧腺苷和脱氧鸟苷衍生物的脱嘌呤风险大大降低。由于省去了用于脱保护的苛刻碱处理，带有对碱不稳定功能的可合成人工类似物的范围得以扩展。
