Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists
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
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
supporting information
p. 5478 - 5483
(2015/01/09)
New macrocyclic bistriazolophanes with thioindigo chromophore
Bi(4-methoxycarbonyl-3-oxothiolan-2-ylidene) derivatives are prepared by oxidative dimerization of 4- oxotetrahydrothiophene-3-carboxylates with either TPAPeNMO or K3[Fe(CN)6]. The products are obtained as mixtures of four diastereoi
Schulz, Marvin,Christoffers, Jens
p. 802 - 809
(2013/07/27)
Methyl 4-Oxothiolane-3-carboxylate and Methyl 2-Methyl-4-oxothiolane-3-carboxylate Anions as Synthetic Equivalents of α-Acrylate and α-Crotonate Anions. Formal Synthesis of Integerrinecic Acid
The base-promoted fragmentation of the C-alkylation products (6a-h) and (8a-e) of methyl 4-oxothiolane-3-carboxylate (4) and methyl 2-methyl-4-oxothiolane-3-carboxylate (5) gave good yields of the α-substituted acrylates (7a-h) and α-substituted crotonate
Baraldi, Pier Giovanni,Guarneri, Mario,Pollini, Gian Piero,Simoni, Daniele,Barco, Achille,Benetti, Simonetta
p. 2501 - 2505
(2007/10/02)
A Novel α-Acrylate Anion Equivalent: A Useful Synthon for α-Substituted Acrylic Esters
An efficient preparation of α-substituted acrylic esters is described, based on the Dieckmann-Michael retrograde reactions of the C-alkylation products of 4-methoxycarbonylthiolan-3-one (1).
Baraldi, Pier Giovanni,Barco, Achille,Benetti, Simonetta,Moroder, Fabio,Pollini, Gian Piero,et al.
p. 1265 - 1266
(2007/10/02)
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