Martin Di Grandi

Associate Professor of Chemistry

Research Interests: synthetic methodology, synthesis of biologically active molecules, and natural products
Offices: Lincoln Center 817C | Rose Hill JMH 538 (office); 542 (lab)
Email: [email protected]
Lincoln Center: 212-636-7141 | Rose Hill: 718-817-4447
 

  • Ph.D., March 1990, New York University
    B.Sc., May 1984, Fordham University

    1. Thioureas as Inhibitors of Herpesviruses.  Herpesviridae is a family of double stranded DNA viruses, of which there are eight that afflict humans, and all are characterized by intermittent periods of infection followed by latency.  Each member of this viral family employs the portal protein, an essential viral protein, for the packaging and release of viral DNA during infection.  More importantly, these proteins possess remarkable structural and functional relatedness across all known members of this virus family.  The focus of this research is to potentially identify one agent that can effectively inhibit the viral replication of multiple herpesviruses.  If true, this agent would not only add to the repertoire of agents for treating herpesvirus infections but given its very different mechanism of action – the lead structures are not nucleosides and will inhibit viral replication by a different means relative to available treatments – these compounds are likely to be equally effective against resistant virus.
    2. 1,2,3,4-Tetrahydroisoquinoline Synthesis.  This project, at its core, involves the ring expansion of activated N-benzylaziridines to 1,2,3,4-tetrahydroiso-quinolines.  More broadly, we have incorporated this chemistry into the synthesis of the tricyclic core ring system of the natural product pancratistatin, an anticancer agent that has been in clinical trials, and presently we are exploring routes to apply this methodology to the total synthesis of the natural product.

    3. The Synthesis of Bipyridyl Ligands as Selective Extractants.  Nuclear waste is currently treated with the Plutonium Uranium Reduction Extraction (PUREX) process, which selectively removes oxidized uranium (VI) and plutonium (IV) but leaves behind minor amounts of actinide and lanthanide ions.  An algorithm designed by Professor Schrier, the Bepler Chair in Chemistry, proposed a bipyridyl extractant as a potential ligand to remove actinides from the remaining nitric acid waste stream, the synthesis of which is currently underway in my lab.

  • Di Grandi, M., Neary, M. C., Corfield, P. W. R. “(4aR*,10bR*)-8,10-Dimethoxy-5-[(4-nitrophenyl)sulfonyl]-3,4,4a,5,6,10b-hexahydrophenanthridine”, International Union of Crystallography Data (IUCr), 2025, 10; (https://iucrdata.iucr.org/x/issues/2025/12/00/hb4549/index.html).

    Di Grandi, M. J., Taylor, B., Corfield, P. W. R. “The crystal structure of 2-[(tert-butyl­diphenylsilyl)­oxy]-1,2-diphenylethan-1-one”, International Union of Crystallography Data (IUCr), 2019, 4; (https://doi.org/10.1107/S2414314619004784).

    Di Grandi, M. J., Bennett, C.; Cagino, K.; Muccini, A.; Suraci, C.; Saba, S. “The Direct Preparation of Amides from Amine Hydrochloride Salts and Orthoesters: A Synthetic and Mechanistic Perspective”, Syn. Comm., 2015, 45(22), 2601-2607.

    Di Grandi, Martin J. “Nazarov-like Cyclization Reactions”, Org. Biomol. Chem., 2014, 12(29), 5331-5345.

    Di Grandi, M.; Olson, M.; Prashad, A. S.; Bebernitz, G.; Luckay, A.; Mullen, S.; Hu, Y.; Krishnamurthy, G.; Pitts, K.; O’Connell, J. “Small Molecule Inhibitors of HIV RT Ribonuclease H”, Bioorg. Med. Chem. Lett., 2010, 20(1), 398-402.

  • Olson, M. W.; Di Grandi, M.; Prashad, A. “Preparation Of Hydantoins Having RNASE Modulatory Activity.” U.S. Pat. Appl. Publ.2005; 16 PP.; US 2005203156 A1.

    Olson, M. W.; Di Grandi, M.; Prashad, A. “Carbamates as HIV Anti-Viral Agents.” U.S. Pat. Appl. Publ. 2005, 15 PP.; US 2005203176 A1.

    Hu, Y.; Sum, F.-W.; Di Grandi, M.; Norton, E. “Preparation Of Anilino-Pyrimidine Phenyl And Benzothiophene Analogs As Protein Kinase Inhibitors For Treating Inflammatory, Autoimmune, Cardiovascular And Other Disease.” U.S. Pat. Appl. Publ. 2007, 36 PP; US 2007244140 A1.

    Olson, M.; Di Grandi, M.; Prashad, A. “Preparation Of 1,2-Dihydroquinoline Derivatives As Inhibitors Of RNASE H And HIV Reverse Transcriptase.” 2009, US Patent 7,553,967, June 30, 2009.

    Olson; M.; Di Grandi, M. “Preparation Of Triazole Derivatives For Treating HIV Infections.” 2009, US Patent 7,563,905, July 21, 2009.

    Levin, J. I.; Hopper, D. W.; Torres, N.; Dutia, M. D.; Berger, D. M.; Wang, X.; Di Grandi, M. J.; Zhang, C.; Dunnick,A.L. “Preparation Of Bridged, Bicyclic Heterocyclic Or Spiro Bicyclic Heterocyclic Derivatives Of Pyrazolo[1,5-A]Pyrimidines as RAF Kinase Inhibitors”, Pct Int. Appl., 2009, 159 PP; WO 2009108838 A1.