Unmet Need

  • Fluorination is vital in drug discovery yet often costly and multi-step
  • Existing routes are essentially de novo syntheses, relying on pre-decorated precursors and often forming elimination side-products
  • The industry is in need for a single-step, site-selective method to stereoconvert substituted fluorinated piperidines late in the workflow.

Our Innovation

  • Epimerization converting cis-fluorinated piperidines to trans in one step
  • Late-stage, site-selective stereochemical editing applicable to drug analogues
  • Selectivity enabled by stereoelectronic/electrostatic effects of fluorine

Advantages

  • Single step access to desired diastereomer; avoids de novo syntheses
  • High stereoselectivity, consistently high yields, broad substrate scope
  • Readily available starting materials; compatible with med-chem diversification

Commercial Opportunity

We are seeking collaboration with pharmaceutical companies and drug discovery partners to apply the stereoconversion for lead optimization, rapid SAR, and candidate acceleration.

Contact in Yissum: Ariela Markel