SYNTHESIS OF PEPTIDES CONTAINING HYDROXYAMINO ACIDS BY THE MIXED ANHYDRIDE METHOD WITHOUT PROTECTING THE HYDROXYL FUNCTIONS
作者:Masaaki Ueki、Toshiyuki Inazu
DOI:10.1246/cl.1982.45
日期:1982.1.5
Dimethylphosphinothioyl(Mpt) mixedanhydrides of N-protected amino acids were found to be isolatably stable and useful for the synthesis of hydroxyamino acid containing peptides without protecting the side-chain hydroxyl functions. They were applied for the solid phase synthesis of an enkephalin analog extended at C-terminal.
发现 N 保护氨基酸的二甲基硫代膦酰 (Mpt) 混合酸酐可分离稳定,可用于合成含羟基氨基酸的肽,而无需保护侧链羟基官能团。它们被应用于在 C 端延伸的脑啡肽类似物的固相合成。
Reactions of 1-substituted 2,2,3,4,4-pentamethylphosphetans with hexafluoroacetone and the 19F nuclear magnetic resonance spectra of the resulting 1,3,2-dioxaphospholans
作者:Robert K. Oram、Stuart Trippett
DOI:10.1039/p19730001300
日期:——
with hexafluoroacetone. The 19F n.m.r. spectra of these adducts over a range of temperatures have given values of the free energies of activation for the pseudorotation processes which place the four-membered ring diequatorial and the 1-substituents apical. The variation in these activation energies with the nature of the 1-substituent is accounted for in terms of the relativeapicophilicity of groups
已经制备了一系列的1-取代的2,2,3,4,4-五甲基膦酸酯,并且在用六氟丙酮处理后将其转化为相应的1,3,2-二氧杂膦酸酯。这些加合物在一定温度范围内的19 F nmr光谱给出了伪旋转过程的活化自由能值,该伪旋转过程使四元环二甲基吡咯和1位取代基位于顶峰。在与1-取代基的性质这些活化能的变化在组既是电负性和的函数的相对apicophilicity方面占p π - d π背键。探索了该假设的一些后果。描述了1,3,2-二氧杂磷杂环戊烷和相关的1,2-氧杂磷杂环戊烷的一些不寻常的反应和异构化。
Highly Enantioselective Allylation of Arylaldehydes Catalyzed by a Silver(I)-Chiral Binaphthylthiophosphoramide
作者:Chun-Jiang Wang、Min Shi
DOI:10.1002/ejoc.200300099
日期:2003.8
diphenylthiophosphoramide L2 prepared from diphenylthiophosphinic chloride and ?-(+)-N-ethyl-1,1'-binaphthyl-2,2'-diamine 2 was used as a catalytic chiral ligand in the siver(I)-catalyzed enantioselectiveallylation reaction of arylaldehydes with allyltribuyltin to furnish high ee (up to 98%) of the homoallylic alcohols.
Novel 4-phenylpiperidines for the treatment of pruritic dermatoses
申请人:——
公开号:US20030078282A1
公开(公告)日:2003-04-24
Novel compounds having general formula (I), and pharmaceutically and veterinarily acceptable salts thereof wherein R 1, R 2, R 3, W, Y 1, Y 2, X, n and y are as defined above and processes for their preparation and intermediate compounds prepared therein. The novel compounds are useful for having utility in the treatment. of pruritic dermatoses including allergic dermatitis and atopy in animals and humans