280765-84-6

Upstream product

• 42921-39-1 methyl 3β-formate-12α-hydroxycholanate 
• 32159-21-0 Cbz-L-pGlu-OH 
• 28050-36-4 3β,12α-Dihydroxy-5β-cholansaeure-methylester 
• 3245-38-3 methyl deoxycholate 
• 75857-94-2 (5S)-N-(benzyloxycarbonyl)-5-methoxycarbonyl-2-pyrrolidinone 

Relevant academic research and scientific papers

Scale-up of trisodium [(3Β,5Β,12α)-3-[[4(S)-4-[bis[2- [bis[(carboxy-kO)methyl]aminokN] 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

Process chemistry involved in the discovery and development routes to trisodium [(3Β,5Β,12α)-3-[[4(S)-4-[bis[2-[bis[(carboxykO) 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.

Blood pool agents for nuclear magnetic resonance diagnostics

The present invention relates to bile acid conjugates and complexes thereof with gadolinium or manganese ions and the salts thereof with physiologically compatible organic or inorganic bases, a process for the preparation thereof and contrastographic diagnostic pharmaceutical compositions containing them.