3, 5-二叔丁基邻苯二酚的过氧化降解偶合反应研究

3, 5-二叔丁基邻苯二酚过氧化氢氧化制备3, 5-二叔丁基邻苯醌时, 发现在氢氧化钾溶液中发生了氧化降解偶合反应, 制得了3, 5-二叔丁基-5-(2, 4-二叔丁基-6-羟基苯氧基)-2-呋喃酮 2; 并对其生成作了较合理的解释。     

Y-Hydroxyphosphonate inducing single-chain antibodies capable of catalyzing soman hydrolysis

A γ-hydroxyphosphonate P6 (O1-methyl-O2-(1, 2, 2-trimethylpropyl)-2-hydroxy-5-nitro-phenyl methylphosphonic acid) which is proposed to be an analog of the transition state in hydrolysis of soman was synthesized. Artificial antigens were obtained by conjugating P6 to the carrier proteins BSA (bovine serum albumin) and LPH (Limulus polyphenus hemocyanin). Mice were immunized with P6-LPH and recombinant single-chain antibody phage display library was constructed. After 4 rounds of panning against P6-BSA and competitive inhibition enzyme immunoassay, more than 70 strains of phage antibodies capable of binding soman were obtained and 11 of them can accelerate the hydrolysis reaction of soman. One of them (EP6) was studied further. Soluble single-chain antibody was prepared and purification was performed by gel filtration and ion exchange chromatography. The kinetic experiment was carried out showing that the turnover number kcatt= 198 min-1 and the rate enhancement kcatkuncat = 122 419. When 0.16 mg · mL-1     

拉呋替丁的波谱学数据和结构确证

对拉呋替丁的氢谱（¹H NMR）、碳谱（¹³C NMR,DEPT）、异核多键相关谱（HMBC）予以解析并进行了报道,对其所有的¹H NMR和¹³C NMR谱信号进行了归属;讨论了红外特征吸收,热差和热重分析;质谱的裂解途径和离子特征也与拉呋替丁的分子结构相符.      

GC-MS测定体内盐酸埃他卡林及药代动力学研究

盐酸埃他卡林具有新颖、独特的抗高血压作用,国家科技部将其列入1035工程重点研究项目.由于该药化学结构及理化性质的特殊性,无法用HPLC及GC等常规方法进行体内药物浓度测定,且该药与多种常用的衍生化试剂难以进行反应,给药代动力学研究带来很大的困难.本文旨在建立灵敏、专一的体内微量药物定量分析方法,评价该药在动物体内的药代动力学性质,保证临床安全合理用药.     

邻二甲胺基苄氯衍生物与取代的2-巯基苯并咪唑 反应规律探索

邻二甲胺基苄氯衍生物1与取代的2-巯基苯并咪唑(2-MBI)(2)反应,可发生S-亲核取代,也可发生N-亲核取代,反应主要取决于1的取代情况,本文对其反应规律进行了探讨。     

γ-羟基膦酸酯诱导梭曼水解单链抗体酶

新型半抗原３－羟基－１－对硝基苯基甲磷酸单频哪基酸酯（Ｐ_６），与血蓝蛋白结合后（Ｐ_６－ＬＰＨ）免疫小鼠，从小鼠脾细胞出发构建单链抗体ｃＤＮＡ文库和噬菌体表面呈现文库．用固相化抗原 Ｐ_６－ＢＳＡ对噬菌体抗体库进行了 ４轮淘选，从中筛选到１１株对梭曼水解有催化作用的单链抗体.对其中一株（ＥＰ_６）进行可溶性抗体的制备，经凝胶过滤和离子交换层析纯化后，ＳＤＳ－ＰＡＧＥ为 ３１ｋｕ的单一条带．酶动力学常数测定其对梭曼水解的催化常数为ｋ_（ｃａｔ）＝１９８ｍｉｎ~(－１)，Ｋ_ｃａｔ／Ｋ_ｕｎｃａｔ＝１２２ ４１９．单链抗体酶ＥＰ６_０．１６ｍｇ·ｍＬ~(－１)与梭曼 ０． １３２ ｍｍｏｌ· Ｌ~（－１）在 ２０℃共温１ｈ后给小鼠背部皮下注射相当于１． １个致死剂量的梭曼， １９只小鼠全部存活，而对照组 １４只小鼠 ３０ ｍｉｎ内全部死亡．小鼠体内抗毒实验显示惊厥潜伏期及死亡时间延长．