2. Academic Validation
  3. Convergent Strategy to Dizocilpine MK-801 and Derivatives

Convergent Strategy to Dizocilpine MK-801 and Derivatives

  • J Org Chem. 2018 Apr 6;83(7):4264-4269. doi: 10.1021/acs.joc.8b00305.
K Harsha Vardhan Reddy 1,  Expédite Yen-Pon 1,  Sylvia Cohen-Kaminsky 2 3,  Samir Messaoudi 1,  Mouad Alami 1
Affiliations

Affiliations

  • 1 Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie , BioCIS, Univ. Paris-Sud, CNRS, University Paris-Saclay , Châtenay-Malabry , F-92296 , France.
  • 2 Inserm UMR_S 999, Hôpital Marie Lannelongue , Le Plessis-Robinson , F-92350 , France.
  • 3 Faculté de Médecine , Univ. Paris-Sud, Université Paris-Saclay , Le Kremlin-Bicêtre , F-94270 , France.
PMID: 29489358 DOI: 10.1021/acs.joc.8b00305
Abstract

A convergent total synthesis of MK-801 has been achieved. Key synthetic transformations include a multicomponent Barbier-type reaction to construct the α-branched amine, a selective Heck α-coupling tactic to generate the exocyclic alkene skeleton, and a late-stage intramolecular hydroamination reaction between the exocyclic alkene and the secondary protected amine. The efficacy of this method was demonstrated by the synthesis of two news analogues substituted on the aromatic rings.

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