201050-21-7Relevant academic research and scientific papers
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists
Azimioara, Mihai,Alper, Phil,Cow, Christopher,Mutnick, Daniel,Nikulin, Victor,Lelais, Gerald,Mecom, John,McNeill, Matthew,Michellys, Pierre-Yves,Wang, Zhiliang,Reding, Esther,Paliotti, Michael,Li, Jing,Bao, Dingjiu,Zoll, Jocelyn,Kim, Young,Zimmerman, Matthew,Groessl, Todd,Tuntland, Tove,Joseph, Sean B.,McNamara, Peter,Seidel, H. Martin,Epple, Robert
, p. 5478 - 5483 (2015/01/09)
Systematic SAR optimization of the GPR119 agonist lead 1, derived from an internal HTS campaign, led to compound 29. Compound 29 displays significantly improved in vitro activity and oral exposure, leading to GLP1 elevation in acutely dosed mice and reduc
The synthesis of 5-substituted 6-oxo-2-piperidinecarboxylic acid derivatives from cyclopentanone-β-ketoesters
Compernolle, Frans,Baens, Nicole,Hoornaert, Georges J.
, p. 433 - 438 (2007/10/03)
Ethyl 2-oxocyclopentanonecarboxylate was converted to 5-substituted 6-oxopiperidinecarboxylic derivatives via a synthetic sequence consisting of a) C-1-alkylation of the cyclopentanone-β-ketoester b) introduction of a protected amino group at the α'-position (C-3) of the cyclopentanone carbonyl group via bromination and substitution with phthalimide c) base promoted ring opening of the disubstuted cyclopentanone-β-ketoester to form the corresponding diester or ester-acid derivatives and d) final deprotection of the amino group with concomitant ring closure to produce the title compounds.
