摘要 |
<p>PURPOSE:To obtain the titled compound in high purity in a short time, by reacting an N-protected L-pyroglutamyl-L-histidine with L-prolinamide under specific condition and subjecting the resultant N-protected thyrotropin-releasing hormone (TRH) to specific treatment. CONSTITUTION:An N-protected L-pyroglutamyl-L-histidine is condensed with L-prolinamide in the presence of a strong acid (e.g. hydrochloric or p- toluenesulfonic acid) using a dialkylcarbodiimide (e.g. dicyclohexylcarbodiimide) to provide an N-protected TRH, which is then catalytically reduced to remove the protecting group. Tartaric acid and acetonitrile are subsequently added to the obtained reaction solution to deposit TRH.tartrate.acetonitrile crystals, which are then dissolved in water to deposit TRH.tartrate.monohydrate crystals and afford the aimed substance.</p> |