Synthesis of a bifunctional monophosphinate DOTA derivative having a free carboxylate group in the phosphorus side chain.

[摘要]：A new bifunctional cyclen-based ligand, 3-[hydroxy({4,7,10-tris[(tert-butoxycarbonyl)methyl]-1,4,7,10-tetraazacycl ododecan-1-yl}methyl)phosphoryl]propanoic acid, was synthesized by alkylation of tri-tert-Bu 1,4,7,10-tetraazacyclododecane-1,4,7-triacetate (t-Bu3DO3A) by Et 3-{ethoxy[(mesyloxy)methyl]phosphoryl}propanoate [MsOCH2P(O)(OEt)CH2CH2CO2Et]. The Et carboxylate group in the side chain was selectively deprotected to obtain the esterified bifunctional ligand. More efficient syntheses of some phosphinopropanoic acid derivs. were devised and the phosphorus alkylation reagent was prepd. starting from hypophosphorus acid or its salt.

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