70336-83-3

Upstream product

• 1454-53-1 ethyl 1-benzyl-4-oxopiperidine-3-carboxylate hydrochloride 
• 41276-30-6 C₉H₁₄O₃NC₆H₅ 

Downstream Products

• 892863-69-3 ethyl 4-amino-1-benzyl-3-piperidinecarboxylate 

Relevant academic research and scientific papers

Development of Novel Anticancer Agents with a Scaffold of Tetrahydropyrido[4,3- d]pyrimidine-2,4-dione

ONC201 is a small molecular anticancer agent currently in multiple Phase II clinical trials. Based on the pharmacophore of ONC201, a series of small molecular compounds with a core structure of tetrahydropyrido[4,3-d]pyrimidine-2,4-dione were designed and synthesized. Preliminary mechanism studies of these compounds indicated that they can inhibit the phosphorylation of AKT and ERK, induce the dephosphorylation of Foxo3a, and promote the expression of TRAIL and the enhancement of activating transcription factor 4 (ATF4) in PC-3 cells. Structure-activity relationship (SAR) studies indicated that modifications of the substituted groups on the core structure can significantly improve the cellular activities of these compounds. The most potent compounds are over 100 times more potent than ONC201 in inhibition of cell growth in a panel of different types of human cancer cell lines.

Synthesis of new trisubstituted 4-aminopiperidines as PAF-receptor antagonists

Two novel classes of 4-aminopiperidines substituted in the 3-position by groups bearing either a carbamate or a ureido function have been synthesized from ethyl 4-oxo-3-piperidinecarboxylate and 3,3′-iminobis(propanenitrile) , respectively. The key step in this synthesis, the reduction of the piperidinic β-enamino ester or nitrile, occurred readily. In contrast to published works, the free primary amines could be isolated from the corresponding β-amino ester or nitrile. Regioselective amidification of the amino group offered two pairs of diastereoisomers which were successfully separated and identified. Measurement of PAF-receptor antagonist activity gave interesting results with an IC50 close to the micromolar. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.