Phosphonate–phosphinate rearrangement

J Org Chem. 2015 Jan 16;80(2):1082-91. doi: 10.1021/jo502567j.

Abstract

LiTMP metalated dimethyl N-Boc-phosphoramidates derived from 1-phenylethylamine and 1,2,3,4-tetrahydronaphthalen-1-ylamine highly selectively at the CH3O group to generate short-lived oxymethyllithiums. These isomerized to diastereomeric hydroxymethylphosphonamidates (phosphate–phosphonate rearrangement). However, s-BuLi converted the dimethyl N-Boc-phosphoramidate derived from 1-phenylethylamine to the N-Boc α-aminophosphonate preferentially. Only s-BuLi deprotonated dimethyl hydroxymethylphosphonamidates at the benzylic position and dimethyl N-Boc α-aminophosphonates at the CH3O group to induce phosphonate–phosphinate rearrangements. In the former case, the migration of the phosphorus substituent from the nitrogen to the carbon atom followed a retentive course with some racemization because of the involvement of a benzyllithium as an intermediate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry*
  • Biochemical Phenomena
  • Lithium Compounds / chemical synthesis*
  • Lithium Compounds / chemistry
  • Molecular Structure
  • Organophosphonates / chemical synthesis*
  • Organophosphonates / chemistry
  • Phenethylamines / chemistry*
  • Phosphoric Acids / chemistry*
  • Tetrahydronaphthalenes / chemical synthesis*
  • Tetrahydronaphthalenes / chemistry

Substances

  • 1,2,3,4-tetrahydronaphthalen-1-ylamine
  • Amides
  • Lithium Compounds
  • Organophosphonates
  • Phenethylamines
  • Phosphoric Acids
  • Tetrahydronaphthalenes
  • phosphoramidic acid