本工作介绍了在胺存在下,通过将Mn(III)与基于聚水杨醛的聚Schiff碱配体络合的胺氧化伯苄基或烯丙基醇,直接制备Schiff碱和肟化合物的新策略。席夫碱-锰(III)配合物)。作为一种新的对环境有益的方案,锰多相聚合物催化系统证明了使用分子氧在乙醇中乙醇的氧化前景广阔。通过2-羟基-5-氯甲基-苯甲醛的缩聚反应合成PSA,然后用2-氨基苯酚处理形成聚合物配体。通过分析方法以及GPC分析来研究PSA的平均分子量。FTIR,UV-Vis,1一步一步地表征了催化剂的形成1 H NMR,TGA,CHN和EDX分析。用ICP-OES仪器研究了金属离子的负载量以及催化剂的浸出量。该催化剂对伯和仲伯苄醇或仲烯丙基醇氧化为羰基化合物具有很高的收率,尤其是在温和,廉价和有效的方法中直接形成亚胺,可以成功地从反应混合物中回收该亚胺并重复使用几次而无需任何操作反应性显着降低。在这项工作中,评估了溶剂,温度
Small molecules for treatment of hypercholesterolemia and related diseases
申请人:Sircar C. Jagadish
公开号:US20050277690A1
公开(公告)日:2005-12-15
The present invention provides compositions adapted to enhance reverse cholesterol transport in mammals. The compositions are suitable for oral delivery and useful in the treatment and/or prevention of hypercholesterolemia, atherosclerosis and associated cardiovascular diseases.
[EN] BACKBONE-CYCLIZED PEPTIDOMIMETICS<br/>[FR] PEPTIDOMIMÉTIQUES À SQUELETTE CYCLISÉ
申请人:POLYPHOR AG
公开号:WO2016162127A1
公开(公告)日:2016-10-13
Novel backbone-cyclized peptidomimetics of the general formula cyclo[-P1-P2-P3-P4-P5-P6-P7-P8-T1-T2-] (I) wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to modulate the GLP-1 receptor. They can be used as medicaments to treat, prevent, or delay the onset of diseases, disorders or conditions in which modulation of the human GLP-1 receptor is beneficial, such as type 2 diabetes. These backbone-cyclized peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
A series of compounds of Formula I are disclosed which are useful in treating viral hepatitus C.
1
披露了一系列的I公式化合物,这些化合物在治疗丙型病毒性肝炎方面是有用的。
[EN] BETA-HAIRPIN PEPTIDOMIMETICS<br/>[FR] PEPTIDOMIMÉTIQUES EN ÉPINGLE À CHEVEUX BÊTA
申请人:POLYPHOR AG
公开号:WO2016150576A1
公开(公告)日:2016-09-29
Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, T, Q., and optionally L being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiellapneumoniae and/or Acinetobacter baumannii and/or Escherichia coli and/or Pseudomonas aeruginosa. They ca n be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
Peptide synthesis by a combination of solid-phase and solution methods I: A new very acid-labile anchor group for the solid phase synthesis of fully protected fragments
作者:M. Mergler、R. Tanner、J. Gosteli、P. Grogg
DOI:10.1016/s0040-4039(00)80405-0
日期:1988.1
The synthesis of a new polymeric support for the preparation of fully protected peptide fragments by the Fmoc/t-butyl method is described. Data for coupling yields and racemization data are given. Cleavage from the resin is performed by very mild acidolysis.1