Shen Shu-bao
2009
Citations
0
Influential Citations
0
Citations
Journal
Chemical Reagents
Abstract
A microwave-irradiation technique was applied to the solid phase synthesis of leuprorelin.The coupling reaction of Fmoc-Arg(Pbf)-OH known as a sterically hindered amino acid with H-Pro-CTC Resin(CTC resin,2-chlorotrityl chloride resin) was investigated.The optimal conditions were as follows:DMF/NMP/THF(at a ratio of 1∶1∶1 by volume) was used as the solvent,HBTU was used as the coupling reagent,the concentration of amino acids was 21 mmol/L,the microwave irradiation time was 3 min,and the reaction temperature was 35 ℃,which was maintained for 6 min.The yield of the target product after coupling of Fmoc-Arg(Pbf)-OH with the H-Pro-CTC resin was improved to reach 84.7%.Finally,the yield of leuprorelin reached 81.3% under optimal conditions.