749885-54-9

Upstream product

• 79981-29-6 (1S,2S)-2-phenylcyclopropylmethyl acetate 
• 17364-45-3 (±)-(1R*,2R*)-(2-phenylcyclopropyl)methyl acetate 
• 35501-81-6 (±)-trans-2-(hydroxymethyl)cyclopropanecarboxylic acid 
• 75-36-5 acetyl chloride 
• 13482-81-0 methyl (±)-trans-2-(hydroxymethyl)cyclopropanecarboxylate 
• 202812-32-6 Acetic acid (1R,2R)-2-phenyl-cyclopropylmethyl ester 

Relevant academic research and scientific papers

ISOQUINOLINES AS INHIBITORS OF HPK1

Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.

NAPHTHYRIDINES AS INHIBITORS OF HPK1

Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

Kinetic Enzymatic Resolution of Cyclopropane Derivatives

The kinetic enzymatic resolution of various cyclopropane derivatives was systematically investigated. The study focused on synthetically useful cyclopropylmethanols (e.g., 18a/j or 19a/j) as well as some rarely investigated cyclopropanols (e.g., 24/25 or 27). The combination of enantioselective catalytic or diastereoselective synthesis of enantiomerically enriched compounds with enzymatic approaches ultimately led to the most convenient route to enantiomerically pure starting materials. Again, this was especially proven for the synthesis of cyclopropanols 18a/j and 19a/j. Key to the successful investigation was to rigorously establish an analytical tool for the analysis of enantiomeric composition of reaction mixtures.

Stereoselective synthesis of novel cyclopropyl analogues of known cysteine protease inhibitors

Efficient synthesis of two novel analogues of some known protease inhibitors, via the isosteric replacement of oxirane/aziridine moiety of the parent compounds by cyclopropane ring, is described.

Stereoselective Synthesis of a Key Precursor of Halicholactone and Neohalicholactone

An efficient synthesis of a known precursor of halicholactone (1a) and neohalicholactone (1b) has been developed using the strategically functionalized key cyclopropane intermediate 2, which in turn has been synthesized via stereoselective cyclopropanation of trans-cinnamyl alcohol in the presence of the chiral dioxaborolane ligand 4. Elaboration of the above bifunctional cyclopropane to the target molecule was achieved in a relatively short reaction sequence and in good overall yield, representing a formal synthesis of the title compounds.