Efficient Synthesis of N-methyl and N-hetero Cyclic Peptoids with Triphosgene as the Coupling Reagent
文献类型：会议论文
| 作者 | Lijing Fang; Zhengyin Pan; Chunlei Wu; Wu Su |
| 出版日期 | 2016 |
| 会议名称 | CPS2016(The 14th Chinese International Peptide Symposium & the 5th Asia-pacific International Peptide Symposium) |
| 会议地点 | 中国南京 |
| 英文摘要 | A range of biological activities, including anticancer, antiviral, antifungal, and immunosuppressive properties [1], have been observed from N-methylated and N-hetero cyclic peptoids. The structural role of N-methyl and N-hetero cyclic residues significantly influences the conformation of peptides, also help to improve the receptor selectivity, metabolic stability, and hydrophobicity.[2] Coupling efficiencies of secondary amines are generally low yielding using conventional coupling agents, typically requiring harsh reaction conditions combined with long coupling time to afford satisfactory incorporation. Our group developed the first synthesis strategy of DNA-binding hairpin pyrrole-imidazole polyamides using BTC-mediated coupling of Boc protected aromatic amino acids.[3] We also automated the synthesis of DNA-binding polyamides using BTC as the coupling agent and showed their compatibility using both Fmoc- and Boc-protected synthesis.[4] We further showcased the superiority of BTC and compatibility as a coupling agent for the synthesis of Coibamide A, resulting in the stereochemical revision of this biologically active natural product. |
| 收录类别 | 其他 |
| 语种 | 英语 |
| 源URL | [http://ir.siat.ac.cn:8080/handle/172644/10817]  |
| 专题 | 深圳先进技术研究院_医药所 |
| 作者单位 | 2016 |
| 推荐引用方式 GB/T 7714 | Lijing Fang,Zhengyin Pan,Chunlei Wu,et al. Efficient Synthesis of N-methyl and N-hetero Cyclic Peptoids with Triphosgene as the Coupling Reagent[C]. 见:CPS2016(The 14th Chinese International Peptide Symposium & the 5th Asia-pacific International Peptide Symposium). 中国南京. |
入库方式： OAI收割
来源：深圳先进技术研究院
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