📜5-氨基乙酰丙酸盐酸盐置于氮体系中,用 Sodium Hydroxide 作为反应溶剂,以95%的收率获得产物3,6-二氢-2,5-吡唑啉胆酸
参考文献:Degradation Mechanism And Stability Of 5‐aminolevulinic Acid
标题:Degradation Mechanism And Stability Of 5‐aminolevulinic Acid
摘要:The Physiological Substance And Precursor Of The Heme Synthesis 5-Aminolevulinic Acid (Ala) Is A Promising Prodrug For Photodiagnosis And Photodynamic Therapy Of Epithelial Tumors,Particularly In Urological And Gynecological Tissues. For The Clinical Use Of This Substance,A Chemically Stable And Sterile Drug Formulation Is Required. In The Present Study,Degradation Mechanism Of Ala In Aqueous Solution And Possibilities To Improve Its Stability Were Examined. A Capillary Electrophoretic Method Was Developed That Was Suitable For The Quantification Of Ala And Of Two Degradation Products. The Intermediate Degradation Product Was 2,5-Dicarboxyethyl-3,6-Dihydropyrazine,Which Was Further Oxidized To 2,5-Dicarboxyethylpyrazine. The Structures Of The Degradation Products Were Proven By (1)H And (13)C Nuclear Magnetic Resonance Spectroscopy. Ala Degradation Was Very Efficiently Inhibited By Adjusting The Ph Of The Aqueous Solution To A Value <5 And By Purging With Nitrogen. Additives Such As Antioxidants Did Not Improve The Ala Stability. These Results Demonstrated That Low Ph Ala Aqueous Solution May Be One Possible Dosage Form To Be Considered For Market Introduction.
DOI:10.1002/1520-6017(200010)89:10<1335::Aid-Jps11>3.0.Co;2-#