Medicinal Chemistry (La Jolla)

Overview

The Medicinal Chemistry Facility at Sanford-Burnham Medical Research Institute is tasked with providing general synthetic and medicinal chemistry resources and expertise to the biomedical research community at the Institute and with external academic partners. Our team is staffed with industry-trained chemists and has a solid track record in all aspects of synthetic problem solving.
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Services

Chemistry Consulting for Projects and Grant Applications

  • Analysis of prior art and chemical landscape

Synthetic and Medicinal Chemistry

  • Synthesis of small molecule reference compounds from milligram to multi-gram scale.
  • Evaluation of structure-activity relationships (SAR), based on biological assay results, and next step decisions for progressing a project forward.
  • Design and synthesis of chemical libraries for hit and lead identification, as well as diversity libraries based on a structural theme.
  • Analog synthesis and lead optimization targeting the improvement of potency, physiochemical, and pharmacokinetic properties.
  • Synthesis of custom organic reagents and synthetic intermediates.

Analytical Chemistry

  • Verification of the structural identity and purity of samples.
  • 1H and 13C NMR with 1D and 2D spectra acquisition and multinuclear capability.
  • HPLC and LC/MS (single quadrupole, triple quadrupole and TOF) analysis.
  • Normal, chiral and reverse phase chromatography separations on analytical and/or preparative scales.
  • High resolution mass spectrometry for accurate mass determination.

Equipment and Resources

The Medicinal Chemistry core in La Jolla occupies approximately 2000 sq. ft. of laboratory space and is equipped with cutting edge synthetic and analytical equipment.

Synthesis Equipment

  • Six 8 ft chemical fume hoods
  • Syrris AFRICA 4 channel microfluidics synthesis system
  • CEM 48 vial microwave system with an Explorer system for automated reaction processing
  • Parr shaker hydrogenation apparatus

Analysis and Purification Equipment

  • Waters automated preparative HPLC AutoPurification system with UV and MS based fraction collection
  • Two Biotage SP4 Flashmaster chromatography units with multi-column functionality and a variable dual wavelength detector
  • Two Shimadzu Discovery preparative HPLC systems with UV detection
  • sco Combiflash automated HPLC with UV detector
  • Waters Acquity LC/MS with ESI-MS and PDA detector for UV and MS interpretation of analytical samples
  • Shimadzu LC/MS 2010EV with ESI-MS and PDA detector
  • Applied Biosystems API3000 for LC/MS-MS studies
  • 400 MHz and 500 MHz Bruker NMR spectrometers with autosamplers
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