scholarly journals Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK

2016 ◽  
Vol 14 (37) ◽  
pp. 8659-8663 ◽  
Author(s):  
Ryan A. Davis ◽  
Kevin Lau ◽  
Sven H. Hausner ◽  
Julie L. Sutcliffe
Keyword(s):  
Peptide Synthesis ◽  
High Purity ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Continuous Process ◽  
Solid Support ◽  
Purification Step ◽  
Phase Synthesis

A rapid, efficient single continuous process for peptide synthesis, cyclization, and radiolabeling on solid-support with a single purification step afforded a high purity radiotracer.

scholarly journals The Breaking Beads Approach for Photocleavage from Solid Support

2020 ◽  
Author(s):  
yasmeen bakhatan ◽  
Israel Alshanski ◽  
Dana Grunhaus ◽  
Mattan Hurevich
Keyword(s):  
Continuous Flow ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
High Energy ◽  
Solid Support ◽  
Phase Synthesis ◽  
Polystyrene Beads ◽  
Magnetic Stirring ◽  
Photolabile Linkers

Photocleavage from polystyrene beads is a pivotal reaction for solid phase synthesis that relies on photolabile linkers. The photocleavage, usually performed by batch irradiation, suffers from incomplete and slow cleavage. To overcome these issues, continuous flow and high-energy lamps are frequently used, but these setups are hazardous, technically challenging, and expensive. We developed a photocleavage approach that relies on a benchtop LED lamp and magnetic stirring. In this approach, we crush the beads instead of keeping their integrity to increase the yield of photocleavage. This approach proved very efficient for photocleavage of protected oligosaccharides.

Overcoming Chemical Challenges in the Solid-Phase Synthesis of High-Purity GnRH Antagonist Degarelix. Part 1.

2019 ◽  
Vol 23 (12) ◽  
pp. 2746-2753 ◽  
Author(s):  
Ivan Guryanov ◽  
Andrea Orlandin ◽  
Angelo Viola ◽  
Barbara Biondi ◽  
Denis Badocco ◽  
...  
Keyword(s):  
High Purity ◽  
Gnrh Antagonist ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis

A New Linker for Solid-Phase Synthesis of Oligonucleotides with Terminal Phosphate Group

2008 ◽  
Vol 73 (1) ◽  
pp. 32-43 ◽  
Author(s):  
Ondřej Pačes ◽  
Zdeněk Točík ◽  
Ivan Rosenberg
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Solid Support ◽  
Phosphate Group ◽  
Phase Synthesis ◽  
Terminal Phosphate Group

Synthesis of a novel cyanoethyl-type linker suitable for the solid-phase synthesis of oligodeoxynucleotides possessing terminal 3'-phosphate group is described. Since the linker is a 2-substituted 2-cyanoethanol, the release of the synthesized oligonucleotide from the solid support is accomplished by β-elimination in the ammonia deprotection step.

Combinatorial Solid-Phase Synthesis of 6-Aryl-1,3,5-triazines via Suzuki Coupling

2011 ◽  
Vol 64 (5) ◽  
pp. 540 ◽  
Author(s):  
Jae Wook Lee ◽  
Hyung-Ho Ha ◽  
Marc Vendrell ◽  
Jacqueline T. Bork ◽  
Young-Tae Chang
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Cross Coupling ◽  
Structural Diversity ◽  
Suzuki Coupling ◽  
Purification Step ◽  
Solid Supports ◽  
Phase Synthesis ◽  
Triazine Derivatives ◽  
Polymer Supported

A synthetic methodology to prepare collections of trisubstituted aryl 1,3,5-triazines with broad structural diversity via Suzuki coupling has been developed. We first optimized the combinatorial derivatization of the triazine core using Suzuki cross-coupling. Second, in order to further expand the methodology for the preparation of negatively charged triazines, we adapted this approach to polymer-supported amino acids and prepared aryl triazines with different charge distribution. With a collection of 160 aryl triazine derivatives in good purities and without any purification step, we proved the viability of this orthogonal scheme for the preparation of triazine libraries using amine/amino acid-captured solid supports and Suzuki cross-coupling.

Synthesis of Casein-Related Peptides and Phosphopeptides. II. The Solid-Phase Synthesis of the Nonphosphorylated Octapeptide Corresponding to Region-14-21 of Bovine β-Casein-A2

1987 ◽  
Vol 40 (8) ◽  
pp. 1389 ◽  
Author(s):  
JW Perich ◽  
NJ Langford ◽  
RB Johns
Keyword(s):  
Mass Spectrometry ◽  
Structural Analysis ◽  
Peptide Synthesis ◽  
Fast Atom Bombardment ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Solid Phase Peptide Synthesis ◽  
Phase Synthesis

The octapeptide CF3C02-. + H2-Glu-Ser-Leu-Ser-Ser-Ser-Glu-Glu-OH (1) was synthesized by the Boc-mode of solid-phase peptide synthesis and hydrogenolytic cleavage of the assembled peptide from the resin support. The 13C n.m.r. spectrum of the octapeptide is presented along with its structural analysis by fast-atom bombardment (f.a.b.) mass spectrometry.

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