882419-75-2Relevant academic research and scientific papers
NITROGEN-CONTAINING HETEROCYCLIC AMIDE COMPOUND AND PHARMACEUTICAL USE THEREOF
-
Paragraph 0287; 0288; 0289; 0290, (2019/08/29)
PROBLEM TO BE SOLVED: To provide a nitrogen-containing heterocyclic amide compound having pyruvate dehydrogenase kinase inhibitory activity, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. SOLUTION: The present invention provides a compound of formula [I-a] or formula [II], or a pharmaceutically acceptable salt thereof (a bond of a dotted line: a single bond or a double bond. X1: C, N, O. X2: C, N. R1a: C1-4 alkyl, C1-4 alkyl carbonyl. R2: halogen, cyano, C1-4 alkyl. A1-A7: C, N, O. A8: C, N. R3, R4: H, C1-4 alkyl. Cy1: C4-6 cycloalkyl or the like. Cy2: C3-6 cycloalkyl or the like. m, t, w: 0, 1. n, r, v: 0, 1, 2.) SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines
Moas-Héloire, Valeria,Renault, Nicolas,Batalha, Vania,Arias, Angela Rincon,Marchivie, Mathieu,Yous, Said,Deguine, Noémie,Buée, Luc,Chavatte, Philippe,Blum, David,Lopes, Luisa,Melnyk, Patricia,Agouridas, Laurence
, p. 15 - 25 (2015/11/23)
In the aim of identifying new privileged structures, we describe the 5-steps synthesis of cyclic guanidine compounds "tetrahydroisoquinoline-iminoimidazolinesg" derived from tetrahydroisoquinoline-hydantoin core. In order to evaluate this new minimal structure and the impact of replacing a carbonyle by a guanidine moiety, their affinity towards adenosine receptor A2A was evaluated and compared to those of tetrahydroisoquinoline-hydantoin compounds.
A new versatile and diastereoselective synthesis of polysubstituted 2-oxopiperazines from naturally occurring amino acids
Reginato, Gianna,Di Credico, Barbara,Andreotti, Daniele,Mingardi, Anna,Paio, Alfredo,Donati, Daniele
, p. 2680 - 2688 (2008/09/16)
A highly stereoselective approach to 1,3,4,5- and 1,3,3′,4,5-polysubstituted 2-oxopiperazines is reported. The method is based on the synthetic elaboration of naturally occurring amino acids to obtain enantiomerically enriched C-5 substituted oxopiperazines, which are further functionalized at C-3 via enolate formation and reaction with electrophiles. Notably, the two nitrogens of the ring can be orthogonally protected.
Efficient preparation of chiral diamines via Red-Al reduction of N-Boc-protected amino acid-derived secondary amides
Voight, Eric A.,Bodenstein, Matthew S.,Ikemoto, Norihiro,Kress, Michael H.
, p. 1717 - 1720 (2007/10/03)
Conditions have been developed for the selective reduction of N-Boc-protected amino acid-derived secondary amides, avoiding the formation of overreduction and cyclic urea byproducts. The method is showcased by the efficient formal synthesis of NK-1 antagonist LY303870.
