1029279-92-2

Upstream product

• 80875-98-5 (2S,3aS,7aS)-perhydroindole-2-carboxylic acid 
• 109523-13-9 (2S,3aS,7aS)-1-(tert-butoxycarbonyl)octahydro-1H-indole-2-carboxylic acid 
• 1029280-03-2 (2S,3aS,7aS)-tert-butyl 2-(phenylcarbamoyl)octahydro-1H-indole-1-carboxylate 

Relevant academic research and scientific papers

R-3-Amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: Design, synthesis, biological evaluation, and molecular modeling

A series of (R)-3-amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives was designed, synthesized, and evaluated as novel inhibitors of dipeptidyl peptidase-4 (DPP-4) for the treatment of type 2 diabetes. Most of the synthesized compounds demonstrated good inhibition activities against DPP-4. Among these, compounds 3e, 4c, 4l, and 4n exhibited prominent inhibition activities against DPP-4, with IC50s of 0.07, 0.07, 0.14, and 0.17 μM, respectively. The possible binding modes of compounds 3e and 4n with dipeptidyl peptidase-4 were also explored by molecular docking simulation. These potent DPP-4 inhibitors were optimized for the absorption, distribution, metabolism, and excretion (ADME) properties, and compound 4n displayed an attractive pharmacokinetic profile (F = 96.3%, t1/2 = 10.5 h).

Synthesis of new perhydroindole derivatives and their evaluation in ruthenium-catalyzed hydrogen transfer reduction

New perhydroindole derivatives were synthesized with good yields and evaluated as chiral ligands in the RuII-catalyzed hydride transfer reduction of acetophenone. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.