Encoded Library Technologies/NCE Molecular Discovery, R&D Medicinal Science and Technology, GlaxoSmithKline, Cambridge, MA, USA.
Methods Mol Biol. 2022;2541:33-37. doi: 10.1007/978-1-0716-2545-3_5.
On-DNA reductive amination (on-DNA aldehyde with amine building blocks) and alkylation (on-DNA amine with aldehyde building blocks) are robust ways to form C-N bond. The large sets of commercially available aldehyde and amine building blocks make reductive amination and alkylation widely used in DEL synthesis.
在 DNA 上进行还原胺化反应(DNA 上的醛与胺砌块反应)和烷基化反应(DNA 上的胺与醛砌块反应)是形成 C-N 键的可靠方法。大量商业可得的醛和胺砌块使得还原胺化和烷基化反应在 DEL 合成中得到广泛应用。