114969-73-2Relevant academic research and scientific papers
Discovery of hydroxy pyrimidine Factor IXa inhibitors
Andreani, Teresa,Chackalamannil, Samuel,Chan, Tin-Yau,Chelliah, Mariappan V.,Clasby, Martin C.,Dwyer, Michael,Eagen, Keith A.,Fried, Steve,Greenlee, William J.,Guo, Zhuyan,Hawes, Brian,Hruza, Alan,Ingram, Richard,Jayne, Charles L.,Keertikar, Kartik M.,Neelamkavil, Santhosh,Reichert, Paul,Xia, Yan
, (2020/06/08)
The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described. Increased selectivity over Factor Xa inhibition was achieved through SAR expansion of the P1 element. Select compounds were evaluated in vivo to assess their plasma levels in rat.
Studies on Pyrimidine Derivatives. XXXIX. Site-Selectivity in the Reaction of 5-Substituted and 4,5-Disubstituted Pyrimidine N-Oxides with Trimethylsilyl Cynanide
Yamanaka, Hiroshi,Sakamoto, Takao,Nishimura, Sumiko,Sagi, Mataichi
, p. 3119 - 3126 (2007/10/02)
The site-selectivity in the modified Reissert-Henze reaction of 5-substituted and 4,5-disubstituted pyrimidine 1-oxides with trimethylsilyl cyanide was examined.The reaction of 5-substituted 4-methoxypyrimidine 1-oxides with trimethylsilyl cyanide gave exclusively 2-pyrimidinecarbonitriles in good yields without exception.On the other hand, the other 5-substituted and 4,5-disubstituted pyrimidine 1-oxides gave mainly 6-pyrimidinecarbonitriles.Keywords--site-selectivity; pyrimidine N-oxide; trimethylsilyl cyanide; Reissert-Henze reasction; pyrimidinecarbonitrile
