Solid-Phase Synthesis of 4,6-Diaryl-3,4-dihydropyrimidine-2(1H)-one- 5-carboxylic Acid Amide Derivatives:  A Biginelli Three-Component Condensation Protocol Based on Immobilized β-Ketoamides

2006 ◽  
Vol 8 (2) ◽  
pp. 153-155 ◽  
Author(s):  
G. Alexander Gross ◽  
Hanns Wurziger ◽  
Andreas Schober
Keyword(s):  
Carboxylic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Acid Amide ◽  
Carboxylic Acid Amide ◽  
Phase Synthesis ◽  
Amide Derivatives

scholarly journals Solid Phase Syntheses of Ferulic Acid Derivatives Acetyl Feruloyl Tyrosine and Acetyl Feruloyl Valyl Tyrosine

2015 ◽  
Vol 9 (1) ◽  
pp. 1-5 ◽  
Author(s):  
Dongxin Zhao ◽  
Li Ma ◽  
Kui Lu ◽  
Juan He
Keyword(s):  
Ferulic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Acid Amide ◽  
Synthesis Method ◽  
Amide Bond ◽  
Peptide Transporter ◽  
Phase Synthesis ◽  
Amide Derivatives ◽  
Fmoc Solid Phase Synthesis

Ferulic acid was used as a common drug for cardia-cerebrovascular disease and leukopenia, but the application of ferulic acid was inhibited by the poor absorption and stability. The improvement of these defects can be realized by modifying ferulic acid by amino acids, because the amido bond can increase the bioavailability and therapeutic effect of some drugs based on the peptide transporter system of mammalian which can transport the peptidyl drugs. The peptidyl derivatives of ferulic acid, namely acetyl feruloyl tyrosine and acetyl feruloyl valyl tyrosine, were synthesized using Fmoc solid-phase synthesis method. The synthesized ferulic acid amide derivatives were purified by RP-HPLC, and characterized by IR, HNMR and ESI-MS. The results indicated that Fmoc solid phase synthesis was a convenient method for the amide bond modification of ferulic acid and the further property research on ferulic acid derivatives.

Parallel Solid-Phase Synthesis and High-Throughput1H NMR Evaluation of a 96-Member 1,2,4-Trisubstituted-pyrimidin-6-one-5-carboxylic Acid Library

2009 ◽  
Vol 11 (3) ◽  
pp. 469-480 ◽  
Author(s):  
Bruce C. Hamper ◽  
Allen S. Kesselring ◽  
Robert C. Chott ◽  
Shengtian Yang
Keyword(s):  
Carboxylic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis

ChemInform Abstract: Zirconyl Chloride Promoted Highly Efficient Solid Phase Synthesis of Amide Derivatives.

ChemInform ◽  
2008 ◽  
Vol 39 (22) ◽  
Author(s):  
Cherkupally Sanjeeva Reddy ◽  
Adki Nagaraj ◽  
Pochampally Jalapathi
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Zirconyl Chloride ◽  
Phase Synthesis ◽  
Highly Efficient ◽  
Amide Derivatives

Synthesis and biological properties of vasopressin analogues containing 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid

1990 ◽  
Vol 55 (4) ◽  
pp. 1099-1105 ◽  
Author(s):  
Zdenko Procházka ◽  
Juris E. Ancans ◽  
Jiřina Slaninová ◽  
Alena Machová ◽  
Tomislav Barth ◽  
...  
Keyword(s):  
Amino Acid ◽  
Carboxylic Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Biological Activities ◽  
Biological Properties ◽  
Phase Synthesis ◽  
Aromatic Residues ◽  
Synthesis Methodology ◽  
Vasopressin Analogues

Solid phase synthesis methodology on a benzhydrylamine resin was used for the synthesis of three analogues of vasopressin with the non-coded amino acid, 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic), in the position 2 ([Tic2, Lys8]VP (I)) and in the position 3 ([Tic3, Lys8]VP (II)). The analogue containing only one Tic in place of both aromatic residues was also isolated (des-Tyr2-[Tic3, Lys8]VP (III)). The biological activities of all analogues were negligible.

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