Scale-Up of Trisodium [(3β,5β,12α)-3-[[4(S)-4-[Bis[2-[bis[(carboxy-kO)methyl]amino-kN]ethyl]amino-kN]-4-(carboxy-kO)-1-oxobutyl]amino]-12-hydroxycholan-24-oato(6-)]gadolinate(3-)], a Gd(III) Complex under Development As a Contrast Agent for MRI Coronary Angiography

Autor:	Daniela Palano, Massimo Visigalli, Pier Lucio Anelli, Giuseppe Manfredi, Marcella Murru, Luciano Lattuada, Marco Sipioni, Pierfrancesco Morosini, Marino Brocchetta
Rok vydání:	2009
Předmět:	Coronary angiography Chemistry Stereochemistry Yield (chemistry) Organic Chemistry Physical and Theoretical Chemistry
Zdroj:	Organic Process Research & Development. 13:739-746
ISSN:	1520-586X 1083-6160
DOI:	10.1021/op900008a
Popis:	Process chemistry involved in the discovery and development routes to trisodium [(3β,5β,12α)-3-[[4(S)-4-[bis[2-[bis[(carboxy-kO)methyl]amino-kN]ethyl]amino-kN]-4-(carboxy-kO)-1-oxobutyl]amino]-12-hydroxycholan-24-oato(6-)]gadolinate(3-)] (B22956/1) starting from l-glutamic acid and (3α,5β,12α)-3,12-dihydroxycholan-24-oic acid is described. The best process is based on seven chemical steps and overcomes difficult purification protocols. Such process has been successfully implemented to prepare multikilogram batches of the target compound in 20% overall yield from (3α,5β,12α)-3,12-dihydroxycholan-24-oic acid.
Databáze:	OpenAIRE
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