CAS: 32644-15-8; (2S)-2-Bromopropanoic Acid

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L-丙氨酸置于硫酸,Potassium Bromide,Sodium Nitrite体系中,用 水 用作溶剂,化学反应 16.0H,反应生成(S)-(-)-2-溴丙酸
参考文献:α-氨基氧基寡肽:一类新型抗癌折叠剂的合成,二级结构和细胞毒性
标题:α-氨基氧基寡肽:一类新型抗癌折叠剂的合成,二级结构和细胞毒性
摘要:α-氨基氧基肽是具有高蛋白水解和构象稳定性的拟肽折叠剂.为了获得对α-氨基氧基寡肽的更好合成途径,我们使用了溶液和固相支持方法的直接组合,并获得了对一组癌细胞显示出显着抗癌活性的寡聚体.我们解决了绕螺旋轴多圈旋转的α-氨氧基肽的第一个x射线晶体结构.晶体结构显示出右旋2 8螺旋构型,每转正好有两个残基,螺旋间距为5.8å.通过二维roesy实验,分子动力学模拟和cd光谱,我们能够确定2 8螺旋是有机溶剂中的主要构象.在水溶液中,α-氨氧基肽在酸性ph下以2 8螺旋构象存在,但随着ph的增加,其二级结构表现出显着变化.在模型膜存在下,最具细胞毒性的α-氨基肽具有增加的吸收2 8螺旋构象的倾向.这表明在作用模式研究中观测到的2 8螺旋构象与膜分解活性之间存在相关性,从而为α-氨氧基肽的折叠特性和生物活性提供了新的见解.
Doi:10.1002/chem.201602521

专利信息

专利号:US-5545568-A
优先权日:1992-09-14
标题:Solid phase and combinatorial synthesis of compounds on a solid support
发明人：ELLMAN JONATHAN A
权利人:UNIV CALIFORNIA
摘要:Methods, compositions, and devices for synthesizing combinatorial libraries of various useful compounds, such as benzodiazepines, prostaglandins, β-turn mimetics and glycerol-derived drugs is described. In order to expediently synthesize such combinatorial libraries of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. This disclosure thus also describes an important extension of solid phase synthesis methods to nonpolymeric organic compounds.

专利号:US-10370409-B2
优先权日:2011-10-25
标题 :Synthesis of libraries of peptide tertiary amides
发明人：KODADEK THOMAS; GAO YU
权利人:SCRIPPS RESEARCH INST
摘要:The present disclosure is directed to a novel class of peptide-like oligomers called peptide tertiary amides (PTAs) and a combinatorial library of PTAs along with synthetic routes for the preparation of large combinatorial libraries of these compounds. The peptide tertiary amides provide an exceptional source of high affinity and selective protein ligands that are useful as tools for biological research and as drug leads, among others.

专利号:WO-2007045192-A1
优先权日:2005-10-18
标题:Glucosaminylmuramic acid derivatives
发明人：LEDVINA MIROSLAV; ZYKA DANIEL; DZOGANOVA MARTINA
权利人:USTAV ORGANICKE CHEMIE A BIOCH; LEDVINA MIROSLAV; ZYKA DANIEL; DZOGANOVA MARTINA
摘要:Disaccharide synthon I (benzyl-2-acetamido-2-deoxy-β-D-glucopyranosyl-(1→4)-2-acetamido-3-0-[1-(R)-carboxyethyl-2-deoxy-α-D-glucopyranoside) and its use for synthesis of 2-acetamido-2-deoxy-β-D-glucopyranosyl-(1→4)-N-acetylmuramic acid VIII and muramyl glycopeptides based on a GMDP molecule IX are described. The synthesis of compound I starts from glycosyl acceptor, the derivative of muramic acid II, which is prepared from compound III by 3-O-alkylation with 2-bromopropionic acid, then following esterification affords compound IV that on splitting off of the isopropylidene group affords the compound V, the partial benzoylation of which affords compound II. Reaction of compound II with 3,4,6-tri-O-acetyl-2-deoxy-2-phthalimido-β-D-glucopyranosyl bromide affords disaccharide VI that is then transformed by sequential removing of the protecting groups, sensitive to alkali, to compound VII, the N-acetylation of which affords compound I. Synthon I is transformed to 2-acetamido-2-deoxy-β-D-glucopyranosyl-(1→4)-N-ace- tylmuramic acid VIII by hydrogenolytic splitting off of benzyl protecting group. Synthon I on reaction with bis(pentafluorophenyl)carbonate affords compound X that on reaction with peptide component affords compound XI, wherein X is a peptide residue. Removing of the protecting groups from compound XI affords muramyl glycopeptide based on a GMDP molecule of general formula IX, wherein X is a peptide residue.

专利号:EP-3567040-B1
优先权日:2013-06-24
标 题 :Method for the preparation of intermediates useful for the synthesis of [1,2,4]-triazolo[4,3-a]pyridines

专利号:US-2014315831-A1
优先权日:2011-10-25
标 题:Synthesis of Libraries of Peptide Tertiary Amides

专利号:WO-2013063296-A1
优先权日:2011-10-25
标题 :Synthesis of libraries of peptide tertiary amides