817562-86-0Relevant academic research and scientific papers
Heterocyclic compound
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Paragraph 1099, (2016/10/08)
The present invention relates to compound (I) or a salt thereof which has a ROR γ t inhibitory action. wherein each symbol is as defined in the specification.
Trivalent Gd-DOTA reagents for modification of proteins
Fisher, Martin J.,Williamson, Daniel J.,Burslem, George M.,Plante, Jeffrey P.,Manfield, Iain W.,Tiede, Christian,Ault, James R.,Stockley, Peter G.,Plein, Sven,Maqbool, Azhar,Tomlinson, Darren C.,Foster, Richard,Warriner, Stuart L.,Bon, Robin S.
, p. 96194 - 96200 (2015/11/24)
The development of novel protein-targeted MRI contrast agents crucially depends on the ability to derivatise suitable targeting moieties with a high payload of relaxation enhancer (e.g., gadolinium(III) complexes such as Gd-DOTA), without losing affinity
Enantiopure bifunctional chelators for copper radiopharmaceuticals - Does chirality matter in radiotracer design?
Singh, Ajay N.,Dakanali, Marianna,Hao, Guiyang,Ramezani, Saleh,Kumar, Amit,Sun, Xiankai
, p. 308 - 315 (2014/05/20)
It is well recognized that carbon chirality plays a critical role in the design of drug molecules. However, very little information is available regarding the effect of stereoisomerism of macrocyclic bifunctional chelators (BFC) on biological behaviors of
Development of a multigram asymmetric synthesis of 2-(R)-2-(4,7,10-tris tert-butylcarboxymethyl-1,4,7,10-tetraazacyclododec-1-yl)-pentanedioic acid, 1-tert-butyl ester, (R)-tert-Bu4-DOTAGA1
Levy, Stuart G.,Jacques, Vincent,Zhou, Kevin Li,Kalogeropoulos, Shirley,Schumacher, Kelly,Amedio, John C.,Scherer, Jonathan E.,Witowski, Steven R.,Lombardy, Richard,Koppetsch, Karsten
experimental part, p. 535 - 542 (2010/04/22)
A process for the multigram asymmetric synthesis of the chiral tetraazamacrocycle 2-(R)-2-(4,7,10-tris tert-butylcarboxymethyl- 1,4,7,10-tetraazacyclododec-1-yl)-pentanedioic acid, 1-tert-butyl ester ((R)-tert-Bu4-DOTAGA, 4) has been devised and demonstrated. The nine-step synthesis features an improved synthesis of 2-(S)-5- oxotetrahydrofuran- 2-carboxylic acid, tert-butyl ester 8, the precursor to the novel alkylating agent (S)-5-benzyl 1-tert-butyl 2-(methylsulfonyloxy) pentanedioate 12, which was used to introduce an orthogonally protected chiral glutarate arm to the 1,4,7,10-tetraazacyclododecane (cyclen) nucleus in high optical purity. Cyclen derivative (R)-t-Bu4-DOTAGA, 4, a key intermediate for the manufacture of a magnetic resonance imaging (MRI) candidate, was produced with high chemical (≥95%) and optical (ee ≥ 97%) purity. The process developed was successfully applied to the kilogram-scale cGMP synthesis of (R)-t-Bu4-DOTAGA.
