Betzing H, Biedermann J
Arzneimittelforschung. 1982;32(8a):916-8.
The systematic syntheses and pharmacological studies of numerous imidazolines aryloxyalkyl-substituted in the 2-position show that substitution of the aryl residue in the 2,6-position by halogen and addition of a side-chain to the alkyl residue results in compounds with marked antihypertensive activity. 2-[1-(2,6-Dichlorphenoxy)-ethyl-2-imidazoline hydrochloride (lofexidine, Lofetensin and Loxacor) exhibits the most marked hypotensive activity. The synthesis and physico-chemical properties of lofexidine are described.
对众多在2-位被芳氧基烷基取代的咪唑啉进行的系统合成及药理研究表明，在2,6-位的芳基残基被卤素取代且在烷基残基上添加侧链会产生具有显著降压活性的化合物。2-[1-(2,6-二氯苯氧基)-乙基]-2-咪唑啉盐酸盐（洛非西定、Lofetensin和Loxacor）表现出最显著的降压活性。文中描述了洛非西定的合成及物理化学性质。
