CAS: 247113-86-6; Fmoc-Phe(4-Cf3)-Oh

上下游产品

1-Fluoro-3-iodobenzene 4-methylbenzotrifluoride (fluorenylmethoxy)carbonyl chloride 4-bromomethyltrifluoromethylbenzene3)-H(1-Bzl)-NH2O-W-F-I-F(4-CF3)-H(1-Bzl)-NH2

📜间氟碘苯置于碳酸甲丙酯,Lithium Hydroxide Monohydrate,碘苯二乙酸,Silver(I) Acetate,Palladium Diacetate,碳酸氢钠,乙二胺体系中,用 四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷,水 用作溶剂,化学反应 38.0H,反应生成Fmoc-L-4-三氟甲基苯丙氨酸
参考文献:使用简单实用的助剂对 α-氨基酸进行配体激活的 β-C-H 芳基化
标题:使用简单实用的助剂对 α-氨基酸进行配体激活的 β-C-H 芳基化
摘要:在过去十年中,人们广泛探索了使用助剂作为导向基团的 Pd 催化的羧酸衍生物的 β-Ch 官能化.与不对称合成中使用最广泛的助剂相比,为 Ch 活化开发的助剂的简单性和实用性仍有待提高.我们之前开发了一种简单的 N-甲氧基酰胺辅助剂来指导 β-Ch 活化,尽管该系统与含有 α-氢原子的羧酸不兼容.在此,我们报道了一种吡啶型配体的开发,该配体克服了 N-甲氧基酰胺助剂的这种限制,从而显着改善了羧酸衍生物,尤其是 α-氨基酸的 β-芳基化.使用这种实用助剂的芳基化应用于非天然氨基酸的克级合成,
Doi:10.1021/ja512690X

专利信息

专利号:WO-2015131100-A1
优先权日:2014-02-28
标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids
发明人：YU JIN-QUAN
权利人:SCRIPPS RESEARCH INST
摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.

专利号:US-11279734-B2
优先权日:2017-12-01
标 题:Solution-phase affinity selection of inhibitors from combinatorial peptide libraries
发明人：PENTELUTE BRADLEY L; TOUTI FAYCAL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., K D of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly). These inventive peptides were rapidly generated and identified using novel methods described herein comprising combinatorial peptide synthesis and/or solution affinity selection.

专利号:US-8338565-B2
优先权日:2008-08-20
标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha
发明人：LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P
权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP
摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.