顺式-1,2-环戊二胺盐酸盐的合成

Synthesis of cis-1,2-Cyclopentyl Amine Hydrochloride

以环戊烯为起始原料,先经碱性高锰酸钾氧化得顺式-1,2-环戊二醇,再经甲磺酰化、胺化得重要中间体顺式-N,N-二(4-甲氧基苄基)环戊基-1,2-二胺,最后经Pd-C/H2还原脱保护制得目标产物顺式-1,2-环戊二胺盐酸盐(1·2HCl),其结构经~1HNMR、^(13)CNMR和ESI-MS确证。该方法原料简单易得、合成路线短、反应条件温和、制备方法成熟,总收率达46.7%,比较适合较大规模的制备。

Cyclopentene was used as the starting material,which was oxidized with alkalinity potassium permanganate to give cis-1,2-cyclopentanediol,followed by methanesulfonylation and amination to afford the important intermediate cis-N,N-bis（ 4-methoxybenzyl） cyclopentyl-1,2-diamine,then deprotection by Pd-C/H2 to give the target compound cis-1,2-cyclopentyl amine hydrochloride（ 1·2HCl） with an overall yield of 46. 7%.The structure was confirmed by 1^HNMR,13^CNMR and ESI-MS.The current method has the advantages of raw material economy,short synthetic route,mild reaction conditions,simple operation and high overall yield,so it is suitable for large-scale production.