N-benzhydryl-glycolamide esters (OBg esters) as carboxyl protecting groups in pept1de synthesis
作者:Muriel Amblard、Marc Rodriguez、Jean Martinez
DOI:10.1016/s0040-4020(01)86014-2
日期:1988.1
N-Benzhydryl-glycolamide esters (OBg esters) of various N-protected amino acids have been synthesized. In order to demonstrate their usefulness in peptide chemistry, the syntheses of For-Met-Leu-Phe-OH (chemiotactic peptide) and Pro-Leu-Gly-NH2 (MIF) have been carried out. OBg esters are compatible with commonly used protectinggroups and are cleanly and selectively removed in mild alkaline conditions
The invention relates to antibacterial amide macrocycles, to methods for the production thereof, and to the use of the same for producing pharmaceuticals for the treatment and/or prophylaxis of illness, especially bacterial infections.
On the use of carboxamidomethyl esters (cam esters) in the synthesis of model peptides. scope and limitations
作者:Jean Martinez、Janine Laur、Bertrand Castro
DOI:10.1016/s0040-4020(01)96451-8
日期:1985.1
protecting group for peptide synthesis was demonstrated. The synthesis of the chemotactic peptide For-Met-Leu-Phe-OH as well as the synthesis of Met-enkephalin using CAM ester as carboxyl terminal protection were performed. These esters showed good stability during acidolytic removal of BOC N-protecting group, during hydrogenolysis of Z N-protecting group and during removal of FMOC N-protecting group. CAM
证明了羧酰胺基甲基酯(CAM酯)作为用于肽合成的羧基保护基的用途。进行了趋化肽For-Met-Leu-Phe-OH的合成以及使用CAM酯作为羧基末端保护的Met-脑啡肽的合成。这些酯在酸解去除BOC N-保护基期间,Z N-保护基的氢解期间和FMOC N-保护基的去除期间显示出良好的稳定性。CAM酯可被NaOH 0.5 N或Na 2 CO 3迅速裂解。但是,当序列中存在天冬氨酸的β-苄基酯时,我们未能成功地选择性除去CAM酯。
Synthesis and Antiviral Study of Acyclic Analogs of 3′-Azido, 3′-Amino, and 3′-Fluoro-3′-deoxythymidine, and of HEPT analogs
作者:Minh-Chau Trinh、Jean-Claude Florent、David S. Grierson、Claude Monneret
DOI:10.1055/s-1994-25609
日期:——
Several new acyclonucleosides have been synthesized from racemic epichlorhydrin or epifluorhydrin. This involves epoxide opening followed by chain elongation with iodomethyl phenyl sulfide and subsequent coupling of the phenylthioacetal with thymine. Deprotection afforded the title compounds 6, 8 and 18, whereas introduction of a phenylthio group at C-6 led to the three HEPT analogs, 13, 19, and 24.
Synthesis of 3′-substituted-2′,3′-dideoxynucleoside analogs as potential anti-aids drugs
作者:Michel Maillard、Abdesslem Faraj、François Frappier、Jean-Claude Florent、David S. Grierson、Claude Monneret
DOI:10.1016/s0040-4039(00)99623-0
日期:1989.1
3′-Amino-3′-deoxythymidine was prepared in six steps and in 67% overall yield from thymidine. Five derivatives of and compound were tested for their anti-HIV activity.