以1-苯甲基-4-哌啶酮合成了4-甲基-N-乙基-N-(4-哌啶基)苯磺酰胺(中间体7),以4-氯苯甲氯为原料,通过溴化及还原合成了5-溴-2-(4-氯苯甲氧基)溴甲基苯(中间体3),通过中间体7和中间体3合成了一种新的小分子化合物4-甲基-N-乙基-N-(N-(5-溴-2-(4-氯苯甲基氧基)苯甲基)-4-哌啶基)苯磺酰胺,对该产物进行了1 H NMR、MS、IR表征及生物活性检测,结果表明该化合物可以作为药物开发的候选化合物.
趋化因子受体CCR5是HIV-1病毒进入人体细胞的主要辅助受体,CCR5拮抗剂可作为一种靶向制剂,以防治人类HIV-1感染.目前,非肽类小分子化合物CCR5拮抗剂的研究占据主导地位.本文以5-溴水杨醛、4-氯苄氯为原料,通过消去、还原及溴化合成了4-溴-2-溴甲基-1-((4-氯苄基)氧)苯(中间体3),以1-苄基-4-哌啶酮合成了N-烯丙基-N-(4-哌啶基)苯甲酰胺,通过中间体3、中间体7合成了一种有望用作CCR5拮抗剂的新的非肽类小分子化合物N-烯丙基-N-(1-(5-溴-2-(对氯苄基氧基)苄基)-4-哌啶基)苯甲酰胺,该产物有一定的生物活性,并对该产物进行了1 H NMR、13C NMR、IR及MS表征.
以5-溴水杨醛、4-氯苄氯为原料,通过消去、还原及溴化合成了4-溴-2-溴甲基-1-((4-溴苄基)氧)苯(3),以哌啶-4-酮合成了N-烯丙基-N-(4-哌啶基)对氯苯甲酰胺(7),通过(3)、(7)合成了一种新的非肽类小分子化合物CCR5拮抗剂N-烯丙基-N-(1-(5-溴-2-((4-氯苄基)氧基)苄基)-4-哌啶基)-4-氯苯甲酰胺(8),并对该产物进行了1 H NMR、13C NMR及MS表征。
We have analyzed the photorefractive（PR） effect of a polymer composite was reported which combines a novel bi-functional poly（N-vinyl）-3-[p-nitrophenylazo]carbazolyl（PVNPAK） and 2,4,7-trinitro-9-fluorenone（TNF）. PVNPAK was synthesized by a post-azo-coupling reaction, with an azo derivative as the electrooptic chromophore and carbazolyl as photoconductive moiety. The asymmetric two-beam coupling gain of 13.9 cm-1 and diffraction efficiency of 1.2% for poled polymer film fabricated using a corona poling are obtained at the wavelength of 647.1 nm, confirming photorefractivity. We interpreted this result as the orientational enhancement, in which the spatial charge field may enhance the modulated orientation of the azobenzen chromophore. It is unexpected that the photorefractive gain of 9.5 cm-1 for the unpoled polymer film also was observed without external field in two-beam coupling（TBC） experiment. This phenomenon is attributed to a light-induced orientational grating when the azobenzene groups are illuminated by polarized light.
