Solid Phase synthesis of Amides Using Mukaiyama'S Reagent

2003 ◽  
Vol 2003 (1) ◽  
pp. 10-11
Author(s):  
Bin Tao ◽  
David W. Boykin
Keyword(s):  
High Purity ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Synthetic Method ◽  
Phase Synthesis ◽  
Mild Conditions

A new solid-phase synthetic method using Mukaiyama's reagent under mild conditions is reported to prepare amides in high purity without purification after cleavage from the resins.

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

ChemInform Abstract: Solid-Phase Synthesis of Glycopeptide Amides Under Mild Conditions: Morphiceptin Analogues.

ChemInform ◽  
1990 ◽  
Vol 21 (20) ◽  
Author(s):  
E. BARDAJI ◽  
J. L. TORRES ◽  
P. CLAPES ◽  
F. ALBERICIO ◽  
G. BARANY ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Mild Conditions

Solid phase synthesis of C-terminal peptide amides under mild conditions

Peptides ◽  
1988 ◽  
pp. 159-161 ◽  
Author(s):  
Fernando Albericio ◽  
Nancy Kneib-Cordonier ◽  
Lajos Gera ◽  
Robert P. Hammer ◽  
Derek Hudson ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Mild Conditions

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 Pictet-Spengler Reaction Updates Its Habits

Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 414 ◽  
Author(s):  
Andrea Calcaterra ◽  
Laura Mangiardi ◽  
Giuliano Delle Monache ◽  
Deborah Quaglio ◽  
Silvia Balducci ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Multicomponent Reaction ◽  
Michael Addition ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Synthetic Method ◽  
Ring Closing Metathesis ◽  
Phase Synthesis ◽  
Acid Catalyzed ◽  
High Yields

The Pictet-Spengler reaction (P-S) is one of the most direct, efficient, and variable synthetic method for the construction of privileged pharmacophores such as tetrahydro-isoquinolines (THIQs), tetrahydro-β-carbolines (THBCs), and polyheterocyclic frameworks. In the lustro (five-year period) following its centenary birthday, the P-S reaction did not exit the stage but it came up again on limelight with new features. This review focuses on the interesting results achieved in this period (2011–2015), analyzing the versatility of this reaction. Classic P-S was reported in the total synthesis of complex alkaloids, in combination with chiral catalysts as well as for the generation of libraries of compounds in medicinal chemistry. The P-S has been used also in tandem reactions, with the sequences including ring closing metathesis, isomerization, Michael addition, and Gold- or Brønsted acid-catalyzed N-acyliminium cyclization. Moreover, the combination of P-S reaction with Ugi multicomponent reaction has been exploited for the construction of highly complex polycyclic architectures in few steps and high yields. The P-S reaction has also been successfully employed in solid-phase synthesis, affording products with different structures, including peptidomimetics, synthetic heterocycles, and natural compounds. Finally, the enzymatic version of P-S has been reported for biosynthesis, biotransformations, and bioconjugations.

Solid-Phase Synthesis of Glycopeptide Amides under Mild Conditions: Morphiceptin Analogues

1990 ◽  
Vol 29 (3) ◽  
pp. 291-292 ◽  
Author(s):  
Eduard Bardají ◽  
Josep L. Torres ◽  
Pere Clapés ◽  
Fernando Albericio ◽  
George Barany ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Mild Conditions

Novel and Efficient Solid-Phase Synthesis of 4,6-Disubstituted 4,5-Dihydro-3(2H)-Pyridazinones

2003 ◽  
Vol 2003 (9) ◽  
pp. 599-600
Author(s):  
Jing Tang ◽  
Xian Huang
Keyword(s):  
High Purity ◽  
Good Yield ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Malonic Ester ◽  
Polymeric Support ◽  
Subsequent Reaction ◽  
Phase Synthesis

The resin-bound 5-monosubstituted cyclic malonic ester 3 was generated and reacted with an α–bromoketone to give the corresponding 5,5-disubstituted cyclic malonic ester resin (4). Subsequent reaction with hydrazine resulted in cyclisation with concomitant cleavage from the polymeric support to release the final products, 4,6-disubstituted 4,5-dihydro-3(2 H)-pyridazinones, in good yield and high purity.

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