A straightforward synthesis and partial hydrolysis of cysteine-derived 2,5-diketopiperazines

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• 作者：Daniela Iannotta ; Nicola Castellucci ; Magda Monari ; Claudia Tomasini
• 刊名：Tetrahedron Letters
• 出版年：2010
• 出版时间：25 August 2010
• 年：2010
• 卷：51
• 期：34
• 页码：4558-4559
• 全文大小：372 K

文摘

A mild and straightforward preparation of cysteine-derived 2,5-diketopiperazines (DKPs) is reported, by cyclization of (R)-2,2-dimethyltetrahydrothiazole-4-carboxylic acid hydrochloride or of (R)-tetrahydrothiazole-4-carboxylic acid hydrochloride, mediated by HBTU and DIEA. One DKP has been characterized by X-ray analysis, while the other has been hydrolyzed to cyclo-Cys-Cys. The preparation of this latter compound has been previously reported to be troublesome and low yielding.