191732-57-7Relevant academic research and scientific papers
Studies toward the duocarmycin prodrugs for the antibody prodrug therapy approach
Li, Lian-Sheng,Sinha, Subhash C.
supporting information; experimental part, p. 2932 - 2935 (2009/07/26)
A tricyclic precursor for the synthesis of the prodrugs of pro-1,2,9,9a-tetrahydrocyclopropa[c]benz-[e]indole-4-one tetramethoxyindolecarboxamide (CBI-TMI) was prepared using the ring-closing metathesis approach. The tricyclic intermediate was converted to an advanced precursor of a CBI-TMI prodrug equipped with a linker presumably suitable for activation using the aldolase catalytic antibody 38C2. An attempted 38C2-catalyzed two-step activation of the hydroxy-pro-CBI intermediate involving retro-aldol and the β-elimination reactions was also examined.
Asymmetric synthesis of the CBI alkylation subunit of the CC-1065 and duocarmycin analogs
Boger, Dale L.,McKie, Jeffrey A.,Boyce, Christopher W.
, p. 515 - 517 (2007/10/03)
Two exceptionally short and effective asymmetric syntheses of N-BOC-CBI are detailed based on an asymmetric hydroboration (80% ee) or Jacobsen epoxidation (92% ee) of a 3,4-dihydrobenzo[f]quinoline followed by direct, transannular spirocyclization for int
