Utility of glycosyl phosphites as glycosyl donors-fructofuranosyl and 2-deoxyhexopyranosyl phosphites in glycoside bond formation
摘要:
The discussion of the ease of generating glycosyl donor properties in the important sugar categories (aldoses, ketoses, deoxy sugars, sugar uronates, and 3-deoxy-2-glyculosonates) implies that phosphites of ketoses and deoxy sugars, respectively, should be valuable donors. This is exhibited for fructofuranosyl phosphite 2 and for 2-deoxyhexopyranosyl phosphites 14a,b which are readily available and generally provide disaccharides in high yields.
含有 Na-T M -磷酸盐的 NASICON 结构的富土混合过渡金属 (T M ) ,即 Na 2 ZrFe(PO 4 ) 3,已使用低成本 Fe 3通过溶胶-凝胶路线制备+为基础的前体。所制备的材料在室温下以所需的菱形 NASICON 结构(空间群: R 3̅ c )结晶。已进行同步加速器 X 射线衍射 (XRD)、透射电子显微镜、X 射线吸收光谱等以确定晶体结构、相关细节、组成和电子结构。从结构特征来看,作为Na 2可能的功能之一FeZr(PO 4 ) 3,Na-嵌入/脱嵌已被检测,这表明通过 Fe 2+ /Fe 3+发生了可逆的电化学 Na-插入/脱出平均电势为 ~2.5 V 的氧化还原。电化学数据和原位同步加速器 XRD 的直接证据表明,在 Na 插入/提取过程中保留了菱形结构,尽管在一定的 Na 含量范围内(即,~2-3 pfu),超过它就会发生菱面体 → 单斜相变。在此范围内,Na
Regioselective synthesis of amphiphilic metoprolol–saccharide conjugates by enzymatic strategy in organic media
作者:Cheng-Zhen Zheng、Jun-Liang Wang、Xia Li、Bo-Kai Liu、Qi Wu、Xian-Fu Lin
DOI:10.1016/j.procbio.2010.07.028
日期:2011.1
group were obtained by using a lipase from porcinepancreas (PPL) in anhydrous tetrachloromethane at 50 °C. Subsequently, alkaline protease from Bacillus subtilis catalyzed highly regioselective acylation of three monosaccharides (glucose, mannose and galactose) and two disaccharides (maltose and sucrose) with N-(5-vinyloxycarbonylpentanoyl)metoprolol in anhydrous pyridine at 50 °C to give metoprolol–saccharide
摘要 开发了一种通过选择性酶促合成方法制备美托洛尔-糖缀合物的有效方案。首先,进行美托洛尔与三种二羧酸二乙烯基酯(琥珀酸二乙烯基酯、己二酸二乙烯基酯和癸二酸二乙烯基酯)的酯交换。考察了有机溶剂、酶来源和酰化试剂对N-(乙烯基氧羰基)美托洛尔合成的影响。通过在 50 °C 的无水四氯甲烷中使用来自猪胰腺 (PPL) 的脂肪酶,获得了一系列具有乙烯基的亲脂性美托洛尔衍生物。随后,来自枯草芽孢杆菌的碱性蛋白酶催化了三种单糖(葡萄糖、甘露糖和半乳糖)和两种二糖(麦芽糖和蔗糖)与 N-(5-乙烯基氧羰基戊酰基)美托洛尔在 50 °C 的无水吡啶中以良好的产率得到美托洛尔-糖缀合物。研究了产物的分配系数。结果表明,与美托洛尔母体药物相比,美托洛尔-单糖和美托洛尔-二糖缀合物的水溶性显着提高,并且美托洛尔-二糖缀合物的水溶性远优于美托洛尔-单糖缀合物。
Biodegradable ocular implants and methods for treating ocular conditions
申请人:Burkstrand J. Michael
公开号:US20080089923A1
公开(公告)日:2008-04-17
Biodegradable ocular implants are described. The ocular implants include a bioactive agent that can be released within the eye to treat an ocular condition or indication. The implants can be used for the administration of a bioactive agent over prolonged periods of time. In some aspects the implants are formed of a matrix of natural biodegradable polysaccharides.
Polypeptide microparticles having sustained release characteristics, methods and uses
申请人:Slager Joram
公开号:US20090022805A1
公开(公告)日:2009-01-22
The invention provides polypeptide microparticles having control release features, particular methods for the preparation of such microparticles, and drug delivery systems that include polypeptide microparticles.
Coatings including natural biodegradable polysaccharides and uses thereof
申请人:Chudzik J. Stephen
公开号:US20070065481A1
公开(公告)日:2007-03-22
Biodegradable coatings and articles that include natural biodegradable polysaccharides are described. The coatings and articles are formed from a plurality of natural biodegradable polysaccharides having pendent coupling groups.
Latent stabilization of bioactive agents releasable from implantable medical articles
申请人:Burkstrand Michael J.
公开号:US20080154241A1
公开(公告)日:2008-06-26
Implantable medical articles comprising natural biodegradable polysaccharides are described. The polysaccharides can provide desirable release properties, and can also be degraded into products that can act as an excipient in the presence of the bioactive agent. In some aspects, the articles are ocular implants formed of a matrix of natural biodegradable polysaccharides. These ocular implants include a bioactive agent that can be released within the eye to treat an ocular condition or indication.