-药物合成数据库

【药物名称】

化学结构式(Chemical Structure):

参考文献No.	537447
标题:	Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives
作者:	Kovalainen, J.T.; Christiaans, J.A.; Kotisaari, S.; Laitinen, J.T.; Mannisto, P.T.; Tuomisto, L.; Gynther, J.
来源:	J Med Chem 1999,42(7),1193

合成路线图解说明: L-Histidine methyl ester (I) was protected as the bis(tritylated) derivative (II) upon treatment with triphenylmethyl chloride and Et3N. Reduction of the ester function of (III) with LiAlH4 afforded alcohol (III), which was coupled with cyclohexylmethyl bromide (IV) in the presence of NaH in DMF, yielding the cyclohexylmethyl ether (V). Finally, cleavage of the trityl protecting groups of (V) with HCl in THF provided the title compound as the dihydrochloride salt.

参考文献No.	546115
标题:	Investigation of the stereospecificity of the histamine H3-receptor with a series of new enantiomeric ligands
作者:	Kovalainen, J.T.; et al.
来源:	15th European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (Sept 6 1998, Edinburgh) 1998,Abst P.34

合成路线图解说明: L-Histidine methyl ester (I) was protected as the bis(tritylated) derivative (II) upon treatment with triphenylmethyl chloride and Et3N. Reduction of the ester function of (III) with LiAlH4 afforded alcohol (III), which was coupled with cyclohexylmethyl bromide (IV) in the presence of NaH in DMF, yielding the cyclohexylmethyl ether (V). Finally, cleavage of the trityl protecting groups of (V) with HCl in THF provided the title compound as the dihydrochloride salt.