Pernak J, Michalak L, Krysinski J, Kuncewicz Z
Poznan University of Technology, Poland.
Arch Pharm (Weinheim). 1995 Jun;328(6):531-3. doi: 10.1002/ardp.19953280611.
DMAP reacts readily with chloromethylcycloalkyl ethers and alpha-chloroethyl alkyl ethers to give stable (1a-1e) and unstable (2a-2h) pyridinium chlorides. Reaction of these chlorides with NaOH produces the corresponding 4-pyridones. All the chlorides synthesized showed antibiotic activity. Particularly high activity against microbes representing cocci, rods, fungi, and bacilli was shown by 1-cyclododecyloxymethyl-4-dimethylaminopyridinium chloride 1d and 1-[(1-dodecyloxy)ethyl]-4-dimethylaminopyridinium chloride 2f.
4-二甲氨基吡啶（DMAP）能与氯甲基环烷基醚和α-氯乙基烷基醚迅速反应，生成稳定的（1a - 1e）和不稳定的（2a - 2h）吡啶鎓氯化物。这些氯化物与氢氧化钠反应生成相应的4-吡啶酮。合成的所有氯化物均显示出抗菌活性。1-环十二烷氧基甲基-4-二甲氨基吡啶鎓氯化物1d和1-[(1-十二烷氧基)乙基]-4-二甲氨基吡啶鎓氯化物2f对代表球菌、杆菌、真菌和芽孢杆菌的微生物表现出特别高的活性。
