Mothes, Celine published the artcileAmino-zinc-ene-enolate cyclization: A short access to cis-3-substituted prolino-homotryptophane derivatives, Category: iodides-buliding-blocks, the main research area is proline substituted asym synthesis amino zinc enolate cyclization AZEE; prolinohomotryptophane chimera asym synthesis AZEE cyclization; enolate cyclization transmetalation iodination protection Negishi cross coupling indole.
Proline chimeras are useful tools for medicinal chem. and/or biol. applications. The asym. synthesis of cis-3-substituted prolines can be easily achieved via amino-zinc-ene-enolate cyclization followed by transmetalation of the cyclic zinc intermediate for further functionalization. Syntheses of prolino-homotryptophane derivatives were achieved through Negishi cross-coupling of the zinc intermediate with indole rings. The use of Pd catalyst derived from Fu’s [(t-Bu3)PH]-BF4 was required to avoid the undesired β-hydride elimination. Optically pure and orthogonally protected compounds were obtained readily usable for peptide synthesis.
Journal of Organic Chemistry published new progress about Cross-coupling reaction (Negishi). 1048039-49-1 belongs to class iodides-buliding-blocks, name is tert-Butyl 5-chloro-3-iodo-1H-indole-1-carboxylate, and the molecular formula is C13H13ClINO2, Category: iodides-buliding-blocks.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com