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 ◽  
...  
2020 ◽  
Vol 24 (2) ◽  
pp. 274-278
Author(s):  
Ivan Guryanov ◽  
Andrea Orlandin ◽  
Angelo Viola ◽  
Barbara Biondi ◽  
Fernando Formaggio ◽  
...  

2016 ◽  
Vol 14 (37) ◽  
pp. 8659-8663 ◽  
Author(s):  
Ryan A. Davis ◽  
Kevin Lau ◽  
Sven H. Hausner ◽  
Julie L. Sutcliffe

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.


2003 ◽  
Vol 2003 (9) ◽  
pp. 599-600
Author(s):  
Jing Tang ◽  
Xian Huang

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.


2009 ◽  
Vol 2009 (5) ◽  
pp. 287-289 ◽  
Author(s):  
Jia-Li Zhang ◽  
Shou-Ri Sheng ◽  
Xue Liu ◽  
Shu-Ying Lin

A novel facile solid-phase organic synthesis of aryl vinyl ethers by reaction of polystyrene-supported β-phenylselenoethanol with phenols under Mitsunobu conditions and subsequent oxidation-elimination with 30% hydrogen peroxide has been developed. The advantages of this method include straightforward operation, lack of odour, good yield and high purity of the products.


2003 ◽  
Vol 2003 (1) ◽  
pp. 10-11
Author(s):  
Bin Tao ◽  
David W. Boykin

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.


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