1446261-69-3

Usage

Uses

Used in Organic Synthesis:
(R)-Benzyl 2-ethynyl-2-methylpyrrolidine-1-carboxylate is used as a building block in organic synthesis for its unique structure and reactivity. Its ethynyl and benzyl functional groups allow for the creation of complex organic molecules, which can be further utilized in various chemical applications.
Used in Pharmaceutical Research:
(R)-Benzyl 2-ethynyl-2-methylpyrrolidine-1-carboxylate is used as a potential candidate in pharmaceutical research due to its structural resemblance to certain bioactive compounds. This similarity may indicate potential pharmacological properties, making it a subject of interest for further study and investigation.

Upstream product

• 220060-08-2 (R)-2-methylpyrrolidine-2-carboxylic acid methyl ester hydrochloride 
• 1330286-50-4 (3S,7aR)-3-(trichloromethyl)tetrahydro-1H,3H-pyrrolo[1,2-c]oxazol-1-one 
• 19734-16-8 diethyl (1-diazo-2-oxo-2-phenylethyl)phosphonate 
• 344-25-2 D-Prolin 

Downstream Products

• 1446261-61-5 (R)-methyl 9-fluoro-11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate 
• 1446261-44-4 (10aR)-2-fluoro-5,8,9,10,10a,11-hexahydro-10a-methyl-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(7H)-one 
• 1446261-52-4 (R)-benzyl 2-((2-amino-6-(methoxycarbonyl)phenyl)ethynyl)-2-methylpyrrolidine-1-carboxylate 
• 1446261-57-9 (R)-benzyl 2-((4-fluoro-2-(methoxycarbonyl)-6-(2,2,2-trifluoroacetamido)phenyl)ethynyl)-2-methylpyrrolidine-1-carboxylate 
• 1446261-55-7 (R)-methyl 11b-methyl-6-oxo-2,3,5,6,11,11b-hexahydro-1H-indolizino[8,7-b]indole-7-carboxylate 
• 1446261-51-3 (R)-methyl 2-(1-(benzyloxycarbonyl)-2-methyltetrahydropyrrol-2-yl)-1H-indole-4-carboxylate 

Relevant academic research and scientific papers

Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development

Poly (ADP-ribose) polymerase (PARP) plays a significant role in DNA repair responses; therefore, this enzyme is targeted by PARP inhibitors in cancer therapy. Here we have developed a number of fused tetra- or pentacyclic dihydrodiazepinoindolone derivatives with excellent PARP enzymatic and cellular PARylation inhibition activities. These efforts led to the identification of pamiparib (BGB-290, 139), which displays excellent PARP-1 and PARP-2 inhibition with IC50 of 1.3 and 0.9 nM, respectively. In a cellular PARylation assay, this compound inhibits PARP activity with IC50 = 0.2 nM. Cocrystal of pamiparib shows similar binding sites with PARP with other PARP inhibitors, but pamiparib is not a P-gp substrate and shows excellent drug metabolism and pharmacokinetics (DMPK) properties with significant brain penetration (17-19%, mice). The compound is currently being investigated in phase III clinical trials as a maintenance therapy in platinum-sensitive ovarian cancer and gastric cancer.