Preparation of N,N-Bis[2-[N',N'-Bis[(Tert-Butoxycarbonyl)Methyl]-Amino]Ethyl-L-Aspartic Acid: An Intermediate in the Synthesis of MRI Contrast Agents

J. C. Amedio Jr. Chemical Development, EPIX Medical, Inc., 71 Rogers St., Cambridge, MA, 02142--1118, USA

G. Van Wagenen Jr Chemical Development, EPIX Medical, Inc., 71 Rogers St., Cambridge, MA, 02142--1118, USA

G. Zavlin Chemical Development, EPIX Medical, Inc., 71 Rogers St., Cambridge, MA, 02142--1118, USA

Albert Gyorkos Hauser Laboratories, 5555 Airport Blvd, Boulder, CO, 80301--2339, USA

S. A. Peterson Hauser Laboratories, 5555 Airport Blvd, Boulder, CO, 80301--2339, USA

Abstract

A preparation of DTPA carboxylic acid 1, a suitable intermediate in the synthesis of MRI contrast agents 2, is described starting from α-tert-butyl-β-benzyl-L-aspartate hydrochloride. In addition, an alternative procedure for the synthesis of bromide 3b is presented.

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Preparation of N,N-Bis[2-[N',N'-Bis[(Tert-Butoxycarbonyl)Methyl]-Amino]Ethyl-L-Aspartic Acid: An Intermediate in the Synthesis of MRI Contrast Agents

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Preparation of N,N-Bis[2-[N',N'-Bis[(Tert-Butoxycarbonyl)Methyl]-Amino]Ethyl-L-Aspartic Acid: An Intermediate in the Synthesis of MRI Contrast Agents

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