多西他赛手性侧链的制备

以苯甲醛(Ⅱ)和S-对甲氧基苯乙胺(Ⅲ)为起始原料,缩合制备N-苯亚甲基-4-甲氧基苯胺(Ⅳ),化合物Ⅳ再与乙酰氧基乙酰氯缩合成四元环,经异丙醚重结晶得到单一手性的(+)-顺式-1-对甲氧基苯基-3-乙酰氧基-4-苯基-2-吖叮啶酮(Ⅴ),再经硝酸铈铵氧化脱去对甲氧基苯乙胺得到(+)-顺式-3-乙酰氧基-4-苯基-2-吖叮啶酮(Ⅶ),然后在碱性条件下脱去乙酰基得到(+)-顺式-3-羟基-4-苯基-2-吖叮啶酮(Ⅷ),最后采用一锅法,化合物Ⅷ先与乙烯基乙醚缩合、再与二叔丁基二碳酸酯缩合直接得到多西他赛手性侧链(Ⅰ),总收率23.4%。该合成方法反应条件温和,反应步骤少,收率高。     

Synthesis and Solid-State Pyrolysis Behavior of POSS Containing Organometallic Polymer with Dicobalt Hexacarbonyl in the Side Chain

POSS containing organometallic polymer (P2-Co) with dicobalt hexacarbonyl in the side chain was synthesized for solid-state pyrolysis to produce magnetic nanoparticles. For comparison, its analogue (P1-Co) without POSS groups was also prepared. After pyrolysis, the nanospheres obtained from P2-Co with POSS groups, had a Co@C–SiOx structure with small and uniform size (~15 nm), and its diameter almost remained unchanged when the pyrolysis temperature increased, showing excellent sinter-resistant properties. However, the nanoparticles obtained from P1-Co sintered seriously at high temperature, and its size was enlarged from 45 to 160 nm, when the pyrolysis temperature increased from 700 to 850 °C. Meanwhile, the obtained nanoparticles all showed good magnetic properties, with the saturation magnetization in the range of 24.0–58.5 emu g^?1, making them promising candidates for the actual applications.     

瑞舒伐他汀侧链的合成

以3-叔丁基二甲硅氧基戊二酸酐和（S）2-羟基-2苯基乙酸苄酯为原料,经过缩合、还原、酯交换、酯化和酯交换制得瑞舒伐他汀侧链（3R）叔丁基二甲硅氧基-6-二甲氧基磷酰基-5-氧代己酸叔丁酯。     

Taxotere侧链的酯类衍生物的合成

本研究选用8个醇,在六甲基二硅基氮烷钠（NaHMDS)的作用下,分别与3－乙氧基乙氧基－4－苯基－2－吖丁啶酮（B）反应,开环生成3－苯基－3－（N－叔丁氧酰氨基）－2－（1－乙氧基乙氧基）丙酸酯（C）,经醋酸水解生成taxotere侧链的衍生物3－苯基－3－（N－叔丁氧酰氨基）－2－羟丙酸酯（D）,这8个酯均为新化合物,其结构经红外,核磁共振光谱及元素分析确定。     

叔丁基头孢克肟侧链酸的合成

以去甲氨噻肟酸乙酯为起始原料,在相转移催化剂聚乙烯醇400存在下一锅法完成水解、醚化反应,精制后得到目标化合物,确定了较优的反应条件,总收率72.8%,纯度98.7%。目标产物的结构均经1HNMR表征。该合成路线原料易得,成本低,操作简单。     

头孢克肟开环侧链酸的合成

以乙酰乙酸叔丁酯为原料,经过肟化、醚化、氯代酯解反应合成了头孢克肟开环侧链酸.比较了肟化反应不同酸化剂对产品的影响,选用乙酸作酸化剂,醚化反应中用溴乙酸甲酯代替氯乙酸甲酯,氯代酯解反应采取低温反应,硫酰氯与醚化物用量摩尔比为2时,反应总收率为53.4%,高于文献值.     

Polycations and their biomedical applications

Polycations are useful delivery vehicles for nucleic acids and proteins. Physicochemical properties, safety, and cost are important design parameters for polycation-enabled controlled release methods. Improvements in the design and biocompatibility of synthetic polycations and complexes thereof are necessary for clinical applications. This review focuses on breakthroughs in the development of biocompatible polycations and their biomedical applications in the past 10 years. First, we summarize current strategies to develop naturally derived and synthetic polycations and describe the most commonly used polycations. Second, we discuss polycation-mediated non-viral gene delivery systems used for tissue engineering and regenerative medicine. Third, we review the development of polycation-mediated self-assembled systems for the delivery of heparin-binding proteins, with an emphasis on translational potential. Finally, we introduce platforms for fabricating polycation-based complexes, including layer-by-layer assembly, polymeric vesicles, polycation-containing microspheres, and approaches to improve the functionality of delivery complexes. With improvements in polycation design, safety, and efficacy, polycation-based controlled delivery is expected to contribute significantly to tissue repair and regeneration applications.     

Transport Behavior of Electrolytes Through Charged Mosaic Composite Membranes

The first part of this article reviews the strong acid/strong base type charged mosaic composite membrane. A template pattern with alternating poly(4-vinylpvridine) (P4VP)/poly(vinyl alcohol) (PVA) lamellae was fabricated upon a microporous membrane by casting of poly[4-vinylpyridine (4VP)-g-vinyl alcohol (VA)] graft copolymer from a water/l-propanol mixture. After a treatment involving the binding of the microporous membrane with the graft copolymer and also domain fixing of the PVA phases, a dilute solution of poly[sodium p-styrenesulfonate (SSS)-g-VA] graft co-polymer/P4VP binary blend was cast on this template surface. After chemical treatments (introduction of a positive charge and domain fixing of ion-exchange regions), we examined the transport of KCl and selective transport of a KCl-sucrose mixture through the charged mosaic composite membrane. The second section reviews the weak acid strong base type charged mosaic composite membrane. In this type, the charged mosaic regions were composed of poly(acrylic acid) (PAA) and quaternized P4VP microdomains. The microstructure of binary blend was observed from scanning electron microscopy (SEM) by wet-etching of films after domain fixing of one component of the binary blend. We examined the transport of KCl and L-phenylalanine through the charged mosaic composite membranes.     

侧链液晶聚硅氧烷的研究进展

侧链液晶聚硅氧烷是一类极具发展前景的新型功能材料,它具有独特的光学、电磁学、黏温特性及较好的机械性能,可用于色谱分离、生物材料、光电信息存贮材料等方面。综述了近年来国内外侧链液晶聚硅氧烷的研究进展,对几种主要类型的侧链液晶聚硅氧烷,即近晶型、向列型、胆甾型以及鱼骨型作了较全面的总结,并对其在色谱分离、生物材料、光电信息存贮材料等方面的应用进行了详细的介绍,最后对其目前的现状作了总结,并对其应用前景进行了展望。     

聚丙烯酸酯类侧链液晶离聚物的合成与表征

以４,４′二羟基联苯为基础合成了一种新型介晶体４－甲基丙烯酸－４′－苄氧基联苯酯及它的均聚物。以偶氮二异丁腈为引发剂,上述介晶单末与甲基丙烯酸通过自由基共聚合反应制备了侧链液晶离聚物Ⅰ和离聚物Ⅱ。用ＦＴＩＲ、＾１Ｈ－ＮＭＲ、ＤＳＣ、热台偏光显微镜、Ｘ射线衍射仪等对其进行了表征。介晶单体的熔点为１５８℃,清亮点为１９６℃,为向列型液晶。均聚物、高聚物Ⅰ和Ⅱ（介晶单体与甲基丙烯酸的摩尔经分别为１：２和     

含PDMS侧链的水性聚氨酯的制备及性能研究

以异佛尔酮二异氰酸酯(IPDI)、聚酯二元醇(PCL)、二羟甲基丙酸(DMPA)、三乙胺(TEA)、乙二胺(EDA)、氨乙基氨丙基聚二甲基硅氧烷(AEAPPDMS)等为原料,采用二次自乳化法,合成系列含PDMS侧链的改性水性聚氨酯(SiPU)。探讨了AEAPPDMS含量对乳液粒径、黏度与涂膜耐水性、机械强度的影响。结果表明:改性后的水性聚氨酯综合性能良好,水性聚氨酯的主链上引入PDMS侧链导致涂膜的吸水率显著下降。     

头孢克肟侧链(甲酯)活性硫酯的合成

从头孢克肟侧链酸(甲酯)合成头孢克肟侧链活性酯,收率82.8%,具有工业生产价值。     

一种头孢地尼侧链酯的制备方法

以(Z)-2-(2-氨基-4-噻唑基)-2-羟基亚胺乙酸乙酯和三苯基甲醇为原料,在碳酸二甲酯溶剂和碳酸二甲酯三氟化硼络合物催化下进行反应,反应完全后减压蒸去溶剂,加甲醇固化析晶,中间产物用片碱水解脱去乙酯,盐酸酸化,得到2-(2-氨基-4-噻唑)-2-(Z)-三苯基甲氧亚胺基乙酸。2-(2-氨基-4-噻唑)-2-(Z)-三苯基甲氧亚胺基乙酸与二硫化二苯骈噻唑,在亚磷酸三乙酯和三乙胺催化下进行酯化得到(Z)-硫代苯骈噻唑-2-(2-氨基-4-噻唑)-三苯甲基氧亚胺基乙酸活性酯,总收率为80.4%。方法操作简单,溶媒低毒易回收,成本低,得到产物纯度高,具有工业化生产前景。     

紫杉醇手性侧链合成与紫杉醇半合成

介绍抗癌药物紫杉醇的几种合成方法,重点阐述紫杉醇手性侧链合成以及应用紫杉醇手性侧链的重要性。同时论述了国内外紫杉醇半合成的研究进展,重点讨论了江苏佩沃特公司研发的对映异构纯的β-内酰胺侧链中间体及其高效的对接路线。     

替比培南匹伏酯及其侧链的合成研究进展

替比培南匹伏酯是一种新型的培南类口服抗菌药物,临床用于治疗儿童感染的肺炎、中耳炎和鼻窦炎等.介绍了替比培南匹伏酯的药理作用,综述了替比培南匹伏酯及其侧链的合成方法,并对其市场前景作了展望.     

头孢菌素及其侧链的开发

介绍了国内外头孢菌素品种的发展概况,重点介绍了头孢菌素侧链产品,指出头孢菌素侧链中间体的生产具有高风险、高回报,国内企业要追求高质量、低成本、注重技术创新与市场开发,开辟国际市场。     

侧链改性的含磷阻燃聚丙烯腈的合成

以N,N'-二甲基甲酰胺为溶剂,将聚丙烯腈(PAN)制成一种侧链上具有高活性噁唑啉基团的改性聚丙烯腈(MPAN),并用傅里叶变换红外光谱(FTIR)、13C核磁共振光谱(NMR)对其结构进行了表征。通过13C NMR积分峰的强度计算得知,聚丙烯腈中大约33%的氰基发生了噁唑啉化反应。在生成的噁唑啉基团中,有1/4的基团在改性的过程中和乙醇胺发生副反应而开环。随后,将制得的MPAN和二苯基磷酸反应制得了侧链上含有磷的改性聚丙烯腈(PMPAN),并用FTIR、31P NMR对反应结果进行了表征。接着,用极限氧指数法(LOI)对PAN和PMPAN的燃烧行为进行了研究,结果显示:PMPAN中磷含量达2.1%时,PMPAN的LOI值为27%。     

阳离子聚合物基因载体:进展与展望

阐述了阳离子聚合物载体用作基因输送的原理,以常见阳离子聚合物,如壳聚糖、聚乙烯亚胺(PEI)、聚(L-赖氨酸)(PLL)和聚甲基丙烯酸-N,N-二甲基氨基乙酯(PDMAEMA)为例,介绍了基因载体的研究进展,最后总结了阳离子聚合物目前存在的问题和对将来的展望。     

疏水侧链型水性聚氨酯缔合型增稠剂的制备与表征

以二醇甘油单油酸酯为扩链剂、聚乙二醇为亲水链段、异佛尔酮二异氰酸酯为连接点合成了疏水侧链型水性聚氨酯缔合型增稠剂(SHEUR)。研究了聚乙二醇的相对分子质量以及二醇甘油单油酸酯的含量对SHEUR性能的影响。对制备的SHEUR进行了红外表征,并进行了表面张力、临界胶束浓度(CMC)以及黏度性能测试。结果表明:SHEUR能够降低溶液表面张力至50 m N/m,在溶液中能够形成胶束;CMC与分子结构有关,降低亲水链段或增加疏水侧链能使CMC值降低,反之,CMC值升高;适当地增加亲水链段长度以及疏水侧链部分的含量,有助于提高SHEUR的自增稠效果。