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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。
To cyclopentene as the starting material, first by alkaline potassium permanganate oxidation of cis-1,2-cyclopentanediol, and then mesylation, amination of the important intermediate cis-N, N -bis (4-methoxybenzyl) cyclopentyl-1,2-diamine, and finally deprotected by Pd-C / H2 reduction to give the target product cis-1,2-cyclopentanediamine hydrochloride (1 · 2HCl), its structure confirmed by ~ 1HNMR, ~ (13) CNMR and ESI-MS. The method has the advantages of simple and easy raw materials, short synthesis route, mild reaction conditions and mature preparation method, and the total yield is 46.7%, which is suitable for larger-scale preparation.