An efficient synthesis of 2-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)morpholine: a potent M1 selective muscarinic agonist

2-(1-Methyl-1,2,5,6-tetrahydropyridin-3-yl)morpholine is useful for synthesizing potent antimicrobials including the arecoline derivatives, phendimetrazine and polygonapholine and was synthesised in nine steps with an overall yield of 36%. Bromination of 3-acetylpyridine and dehydration of a diol with cyclization were pivotal to the success of the strategy.     

液相色谱法测定槟榔饮片中槟榔碱含量的不确定度评定

根据《测量不确定度评定与表示》对液相色谱法测定槟榔饮片中槟榔碱含量的不确定度进行评定。通过分析得出,体积类不确定度是主要影响因素。分析结果表明,当槟榔饮片中槟榔碱含量为0．58％时,其扩展不确定度为0．02％（k=2）     

Synthesis and Their Endothelium Vascular Relaxation of Arecoline Derivatives Containing Oxadiazoline

Ten novel 1,1-dimethyl-3-(2-or 5-aryl-4-acetyl-2,3-dihydro-1,3,4-oxadiazoline-5-or-2-yl)-1,2,5,6-tetrahydropyridinium iodides were synthesized from starting materials nicotinalde-hyde or nicotinic acid by two different synthetic methods respectively. The preliminary bioactive tests indicate som compounds exhibit potent relaxing effect on endothelial cells, comparable to Ach or arecoline.     

Hydroxy- und Epoxyderivate von Arecolin

The epoxides10,12, and13 were synthesized from the basic olefines9 and11 by epoxidation of the corresponding trifluoroacetates. Base catalyzed rearrangement of12 and13 yielded the product14. The relative configurations of12 and13 were determined by¹H-NMR spectroscopy.

Herrn Prof. Dr.Kurt L. Komarek mit den besten Wünschen zum 60. Geburtstag gewidmet.     

A new matrix for analyzing low molecular mass compounds and its application for determination of carcinogenic areca alkaloids by matrix-assisted laser desorption ionization time-of-flight mass spectrometry

Arecoline is the main alkaloid present in the areca nut (or betel nut) and it has central nervous system effects. Its pharmacological activities induce the constriction of the bronchial smooth muscles, and stimulation of the lacrimal and intestinal glands. Chewing areca nut is harmful to health because this habit may increase the risk of the development of oral cancer. In this study, a fast method was provided for the determination of areca alkaloids by matrix-assisted laser desorption ionization (MALDI) mass spectrometer with a time-of-flight (TOF) analyzer. Traditionally the MALDI-TOF method was not suitable for the analysis of small molecular weight (m/z < 600) compounds because of the high background of the matrix. In this study, a new matrix was utilized to decrease the background interference effectively. After simple sample preparation, 1 μL sample supernatant was mixed with 1 μL matrix and then deposited on the target plate. This new matrix was also used to test the MALDI imaging experiment. Application of this MALDI-TOF method for trace analysis of arecoline by this new matrix in human plasma at sub μM level proved workable.