Synthetic study on novel immunosuppressant KF20444

Bioorg Med Chem. 2001 Dec;9(12):3273-86. doi: 10.1016/s0968-0896(01)00238-3.

Abstract

The two new synthetic routes to 6,7-dihydro-10-fluoro-3-(2-fluorophenyl)-5H- benzo[6,7]cyclohepta[1,2-b]-quinoline-8-carboxylic acid (1), a novel immunosuppressant KF20444, are described. The seven-membered ring construction from 2-[4-(2-fluorophenyl)phenyl]-3-(2-carboxyethyl)-4-chloromethyl-6-fluoroquinoline (17c) was achieved by intramolecular Friedel-Crafts reaction under acidic conditions as the key step. Subsequently, the oxidation of 4-chloromethyl group followed by reduction of carbonyl group on the seven-membered ring afforded 1. This route provides a new method for the synthesis of 1.

MeSH terms

  • Biochemistry / methods*
  • Biphenyl Compounds / chemical synthesis*
  • Immunosuppressive Agents / chemical synthesis*

Substances

  • Biphenyl Compounds
  • Immunosuppressive Agents
  • KF 20444