130707-81-2

Upstream product

• 67-56-1 methanol 
• 5600-62-4 4-(4-nitrophenyl)butanoic acid 
• 294-90-6 1,4,7,10-tetraazacyclododecan 
• 130707-80-1 d,l-2-bromo-4-(4-nitrophenyl)butanoic acid methyl ester 

Downstream Products

• 130707-75-4 α-[2-(4-aminophenyl)ethyl]-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid 
• 130707-73-2 α-[2-(4-nitrophenyl)ethyl]-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid, 1,4,7,10-tetramethyl ester 
• 596121-76-5 C₄₀H₆₁N₅O₁₆ 
• 259088-63-6 1,4,7,10-tetraaza-N-(1-carbomethoxy-3-(4-nitrophenyl)propyl)-N',N'',N'''-tris(acetic acid, ethyl ester)cyclododecane 

Relevant academic research and scientific papers

Oligomers of gadolinium chelates, their applicationascontrast products in magnetic resonance imaging and their synthesis intermediates

The invention relates to high-relaxivity macrocyclic gadolinium chelate oligomers of formula [in-line-formulae]W-(A)m[/in-line-formulae] in which W, A and m are as defined in claim 1, and their use as a blood pool contrast product for magnetic resonance imaging.

Improved synthesis of the bifunctional chelating agent 1,4,7,10- tetraaza-N-(1-carboxy-3-(4-nitrophenyl)propyl)-N',N'',N'''-tris(acetic acid)cyclododecane (PA-DOTA)

A concise synthesis of the bifunctional chelating agent 1,4,7,10- tetraaza-N-(1-carboxy-3-(4-nitrophenyl)propyl)-N','',N'''-tris(acetic acid)cyclododecane (PA-DOTA) is reported. Difficulties involving the production of partially alkylated products and the

Macrocyclic tetraazacyclododecane conjugates and their use as diagnostic and therapeutic agents

A group conjugates having a functionalized polyaminocarboxylate chelant that form complexes with rare earth-type metal ions, covalently attached to an antibody or antibody fragment, can be used for therapeutic and/or diagnostic purposes.

Unexpected Selectivity in the Alkylation of Polyazamacrocycles

Reaction of equivalent amounts of free base polyazamacrocycles with an alkyl halide in a nonpolar, aprotic solvent affords the mono-N-alkylation product as its monohydrohalide salt in high yield with excellent selectivity.This unexpected selectivity has been explained in terms of the high affinity of the alkylated product for a single proton which attenuates the nucleophilicity of the remaining nitrogen atoms.Selectivity is dependent upon a number of factors including macrocycle ring size, solvent polarity, and the steric nature of the electrophile.The approach has been allowed for a short, convergent route to bifunctional lanthanide chelators which are useful in therapeutic applications.

Process for preparing mono-n-alkylated polyazamacrocycles

The invention relates to a novel process to prepare selectively mono-N-alkylated polyazamacrocycles which requires an electrophile with between about one and five equivalents of a suitable macrocycle in a solvent which will not promote a proton transfer.