- Probing the Reactivity of 2,4-Dichlorofuro[3,4-d ]pyrimidin-7-one: A Versatile and Underexploited Scaffold to Generate Substituted or Fused Pyrimidine Derivatives
-
Herein, we describe the results of our investigation on the chemical reactivity and versatility of a poorly explored scaffold: 2,4-dichlorofuro[3,4-d ]pyrimidin-7-one (3). Highly functionalized pyrimidines can be obtained with a divergent approach by reacting the key intermediate 3 with different amine nucleophiles under carefully controlled reaction conditions. The set-up of a microwave-Assisted one-pot, two-or three-step protocol to rapidly generate 2,4,5,6-Tetrasubstituted or fused pyrimidines is also reported.
- Costantino, Gabriele,Martina, Maria Grazia,Radi, Marco,Vincetti, Paolo
-
supporting information
p. 2010 - 2014
(2019/10/22)
-
- Discovery of P2X3 selective antagonists for the treatment of chronic pain
-
Purinergic receptor P2X3 has been linked to analgesia in a number of pre-clinical models of pain, and is expressed in the human pain perception pathway. Only few P2X3-selective antagonists have been reported to date. This Letter describes the SAR and in vivo analgesic profile of a novel scaffold of selective P2X3 antagonists.
- Cantin, Louis-David,Bayrakdarian, Malken,Buon, Christophe,Grazzini, Eric,Hu, Yun-Jin,Labrecque, Jean,Leung, Carmen,Luo, Xuehong,Martino, Giovanni,Paré, Michel,Payza, Kemal,Popovic, Nirvana,Projean, Denis,Santhakumar,Walpole, Christopher,Yu, Xiao Hong,Tomaszewski, Miros?aw J.
-
scheme or table
p. 2565 - 2571
(2012/05/05)
-
- DIHYDROFUROPYRIMID1NE COMPOUNDS
-
The present invention provides mTOR inhibitors of the formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods of making the compounds and intermediates thereof; and methods of using the compounds.
- -
-
Page/Page column 21
(2012/08/07)
-
- DIHYROFUROPYRMINDINE COMPOUNDS
-
The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods of making the compounds and intermediates thereof; and methods of using the compounds.
- -
-
Page/Page column 10
(2011/02/18)
-
- OXO-HETEROCYCLE FUSED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
-
Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
- -
-
Page/Page column 75
(2011/01/05)
-