CGP-40774, JBT-3002, JENACT

Chemical Name: 14(R)-(Dodecanoyloxy)-4,9,17-trioxo-10(R)-(pentadecanamido)-7(S)-[N-(2-sulfoethyl)carbamoyl]-16-oxa-12-thia-3,8-diazaoctacosane-1-sulfonic acid disodium salt; S-[2(R),3-Bis(dodecanoyloxy)propyl]-N-(hexadecanoyl)-L-cysteinyl--L-glutamamic acid N1,N5-bis(2-sulfoethyl)amide disodium salt
CAS No. 150496-14-3, 150575-90-9 (free acid)
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:The condensation of N-(benzyloxycarbonyl)-L-glutamic acid bis(2,4,6-trichlorophenyl) ester (I) with taurine (II) in the presence of NaOH provided diamide (III).After deprotection of the benzyloxycarbonyl group of (III) by hydrogenolysis over Pd/C,the resulting amine (IV) was coupled with N-palmitoyl-S-(2,3-dilauroyloxypropyl)cysteine (V) using N,N'-dicyclohexylcarbodiimide and N-hydroxynorbornan-2,3-dicarboximide (A) to furnish the title compound.