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Direct synthesis of 1,1'-[1,4-phenylenebis(methylene)]-bis- 1,4,8,11-tetraazacyclotetradecane octahydrochloride (AMD 3100) without the use of protecting groups. | LitMetric

A four-step synthesis of the title compound starting from methyl acrylate, ethylenediamine, and dimethyl malonate is reported. The synthesis can be run on a multigram scale and is operationally simple. The use of protecting groups is avoided by utilizing the trioxocyclam as the key coupling intermediate.

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http://dx.doi.org/10.1021/jo030146rDOI Listing

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