1-[二-(4-氟苯)甲基]-4-取代哌嗪是一类重要的药物中间体,随着哌嗪环4-位引入不同的取代基可以产生不同的生物活性,如治疗偏头痛药物氟桂利嗪、洛美利嗪,抗氧化剂[1,2]、钙拮抗剂[3]、癌症治疗中多种抗药性的调节剂(modulator of MD... 1-[二-(4-氟苯)甲基]-4-取代哌嗪是一类重要的药物中间体,随着哌嗪环4-位引入不同的取代基可以产生不同的生物活性,如治疗偏头痛药物氟桂利嗪、洛美利嗪,抗氧化剂[1,2]、钙拮抗剂[3]、癌症治疗中多种抗药性的调节剂(modulator of MDR)[4,5]等;此外,含有酰基结构单元的哌嗪衍生物具有降压活性,如哌唑嗪等[6,7].因此根据药学上的拼合原理,我们以哌嗪为母体,采用哌嗪环先引入二-(4-氟苯)甲基后引入酰基的策略,设计合成了九个未见文献报道的1-[二-(4-氟苯)甲基]-4-酰基取代哌嗪类衍生物(4a～4i),如下图所示,其结构用红外、质谱、核磁、元素分析进行了分析表征,并总结了其波谱特征.此类化合物对治疗偏头痛和高血压的活性研究正在进行之中.……展开更多
Owing to having very strong bioactivity, oligo-peptides can be used as the medication or the pre-medication and become the studying focus now. Existing methods for synthesizing oligo-peptides included liquid phase pep...Owing to having very strong bioactivity, oligo-peptides can be used as the medication or the pre-medication and become the studying focus now. Existing methods for synthesizing oligo-peptides included liquid phase peptide synthesis, solid phase peptide synthesis and enzymatic peptide synthesis. In this paper, a new method for synthesizing oligo-peptides by phosphorus oxychloride activation was reported. With the assistance of phosphorus oxychloride, the phosphorylation of L-valine could take place and then was assembled into oligo-peptides, which were analyzed by electrospray ionization mass spectrometry(ESI-MS). On quenching with methanol, the reaction mixtures, which were produced under different reaction conditions, yielded the corresponding peptide methyl esters. Moreover, we found that, as the reaction conditions such as reaction time, solvent and temperature were changed, the length of peptides changed. And the length of peptides could be controlled by changing the reaction conditions.展开更多
文摘 1-[二-(4-氟苯)甲基]-4-取代哌嗪是一类重要的药物中间体,随着哌嗪环4-位引入不同的取代基可以产生不同的生物活性,如治疗偏头痛药物氟桂利嗪、洛美利嗪,抗氧化剂[1,2]、钙拮抗剂[3]、癌症治疗中多种抗药性的调节剂(modulator of MDR)[4,5]等;此外,含有酰基结构单元的哌嗪衍生物具有降压活性,如哌唑嗪等[6,7].因此根据药学上的拼合原理,我们以哌嗪为母体,采用哌嗪环先引入二-(4-氟苯)甲基后引入酰基的策略,设计合成了九个未见文献报道的1-[二-(4-氟苯)甲基]-4-酰基取代哌嗪类衍生物(4a～4i),如下图所示,其结构用红外、质谱、核磁、元素分析进行了分析表征,并总结了其波谱特征.此类化合物对治疗偏头痛和高血压的活性研究正在进行之中.……
文摘Owing to having very strong bioactivity, oligo-peptides can be used as the medication or the pre-medication and become the studying focus now. Existing methods for synthesizing oligo-peptides included liquid phase peptide synthesis, solid phase peptide synthesis and enzymatic peptide synthesis. In this paper, a new method for synthesizing oligo-peptides by phosphorus oxychloride activation was reported. With the assistance of phosphorus oxychloride, the phosphorylation of L-valine could take place and then was assembled into oligo-peptides, which were analyzed by electrospray ionization mass spectrometry(ESI-MS). On quenching with methanol, the reaction mixtures, which were produced under different reaction conditions, yielded the corresponding peptide methyl esters. Moreover, we found that, as the reaction conditions such as reaction time, solvent and temperature were changed, the length of peptides changed. And the length of peptides could be controlled by changing the reaction conditions.
