158741-16-3Relevant articles and documents
One Stone Two Birds—Enantioselective Bimetallic Catalysis for α-Amino Acid Derivatives with an Allene Unit
Huo, Xiaohong,Ma, Shengming,Xiao, Junzhe,Xu, Haibo,Zhang, Wanbin
supporting information, p. 1958 - 1964 (2021/05/31)
A highly enantioselective 2,3-allenylation of acyclic and cyclic α-imino carboxylates via a synergistic bimetallic Pd/Cu catalysis with the same commercially available (R,Rp)-iPr-FOXAP (also as Phosferrox, (R,R)-[2-(4’-i-propyloxazolin-2’-yl)ferrocenyl]diphenyl phosphine) ligand for both metals affording optically active 2,3-butadienyl α-amino acid derivatives in high to excellent yields with excellent enantioselectivities has been developed. The synthetic versatility of this reaction has been demonstrated by gram-scale synthesis, a catalytic enantioselective synthesis of naturally occurring (S)-2-amino-4,5-hexadienoic acid A, and conversions to several useful chemicals, such as optically active α-amino acids, β-amino alcohols, potential chiral oxazoline ligands bearing an allenic moiety, and bicyclic ketone compounds. A mechanism involving the roles of two metals and the single chiral ligand has been extensively studied based on the isolation of key palladium pre-catalyst and control experiments.
Macrocyclic Modulators of the Ghrelin Receptor
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Paragraph 0574; 0575, (2018/05/03)
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
The Synthesis and Thymidylate Synthase Inhibitory Activity of L-γ-L-Linked Dipeptide and L-γ-Amide Analogues of 2-Desamino-2-methyl-N10-propargyl-5,8-dideazafolic Acid (ICI 198583)
Bisset, Graham M. F.,Bavetsias, Vassilios,Thornton, Timothy J.,Pawelczak, Krzysztof,Calvert, A. Hilary,et al.
, p. 3294 - 3302 (2007/10/02)
Sixteen γ-linked dipeptide and four L-Glu-γ-amide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583) have beensynthesized and evaluated as inhibitors of thymidylate synthase (TS).Z-blocked L-Glu-γ-L-linked dipepti
