902765-47-3Relevant articles and documents
One-Pot Cascade Heterocyclization of γ- And β-Ketomalononitriles to 2,4-Dichloro-Substituted Pyrano[2,3- d]pyrimidines and Furo[2,3- d]pyrimidines Mediated by Triphosgene and Triphenylphosphine Oxide
Li, Zhen-Hua,Jiang, Zhi-Jiang,Shao, Qiao-Ling,Qin, Jin-Jing,Shu, Qiang-Feng,Lu, Wen-Hao,Su, Wei-Ke
, p. 6423 - 6431 (2018)
A one-pot cascade heterocyclization strategy has been developed for the synthesis of 2,4-dichloro-substituted pyrano[2,3-d]pyrimidines and furo[2,3-d]pyrimidines from linear γ- and β-ketomalononitriles using triphosgene and triphenylphosphine oxide. The reaction afforded synthetic useful products with moderate to good yields, bypassing the conventional harsh conditions of chlorination. The mechanistic study revealed that the reaction proceeded with a non-isocyanate route, and the second step may conduct in a triphenylphosphine oxide-catalyzed manner.
2,4-Diaminothienopyrimidines as orally active antimalarial agents
González Cabrera, Diego,Le Manach, Claire,Douelle, Frederic,Younis, Yassir,Feng, Tzu-Shean,Paquet, Tanya,Nchinda, Aloysius T.,Street, Leslie J.,Taylor, Dale,De Kock, Carmen,Wiesner, Lubbe,Duffy, Sandra,White, Karen L.,Zabiulla, K. Mohammed,Sambandan, Yuvaraj,Bashyam, Sridevi,Waterson, David,Witty, Michael J.,Charman, Susan A.,Avery, Vicky M.,Wittlin, Sergio,Chibale, Kelly
, p. 1014 - 1022 (2014/03/21)
A novel series of 2,4-diaminothienopyrimidines with potential as antimalarials was identified from whole-cell high-throughput screening of a SoftFocus ion channel library. Synthesis and structure-activity relationship studies identified compounds with potent antiplasmodial activity and low in vitro cytotoxicity. Several of these analogues exhibited in vivo activity in the Plasmodium berghei mouse model when administered orally. However, inhibition of the hERG potassium channel was identified as a liability for this series.
THIENO [2,3-D] PYRIMIDINE COMPOUNDS AS INHIBITORS OF ADP-MEDIATED PLATELETS AGGREGATION
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Page/Page column 78, (2008/06/13)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I): wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.