67264-28-2Relevant articles and documents
Mn(III)-mediated phosphonation-azidation of alkenes: A facile synthesis of β-azidophosphonates
Xu, Jian,Li, Xueqin,Gao, Yuzhen,Zhang, Liangliang,Chen, Weizhu,Fang, Hua,Tang, Guo,Zhao, Yufen
, p. 11240 - 11243 (2015)
A new and general method for the synthesis of β-azidophosphonates has been achieved through Mn(OAc)3-mediated radical oxidative phosphonation-azidation of alkenes. The starting materials of P(O)-H compounds, alkenes, and azidotrimethylsilane are stable and cheap. This method can be easily adapted for large-scale preparation.
Pharmacophore Mapping of Thienopyrimidine-Based Monophosphonate (ThP-MP) Inhibitors of the Human Farnesyl Pyrophosphate Synthase
Park, Jaeok,Leung, Chun Yuen,Matralis, Alexios N.,Lacbay, Cyrus M.,Tsakos, Michail,Fernandez De Troconiz, Guillermo,Berghuis, Albert M.,Tsantrizos, Youla S.
, p. 2119 - 2134 (2017/03/17)
The human farnesyl pyrophosphate synthase (hFPPS), a key regulatory enzyme in the mevalonate pathway, catalyzes the biosynthesis of the C-15 isoprenoid farnesyl pyrophosphate (FPP). FPP plays a crucial role in the post-translational prenylation of small GTPases that perform a plethora of cellular functions. Although hFPPS is a well-established therapeutic target for lytic bone diseases, the currently available bisphosphonate drugs exhibit poor cellular uptake and distribution into nonskeletal tissues. Recent drug discovery efforts have focused primarily on allosteric inhibition of hFPPS and the discovery of non-bisphosphonate drugs for potentially treating nonskeletal diseases. Hit-to-lead optimization of a new series of thienopyrimidine-based monosphosphonates (ThP-MPs) led to the identification of analogs with nanomolar potency in inhibiting hFPPS. Their interactions with the allosteric pocket of the enzyme were characterized by crystallography, and the results provide further insight into the pharmacophore requirements for allosteric inhibition.
Synthesis of β-amino phosphonates in one-pot procedure
Jang, Won Bum,Shin, Won Suk,Lee, Kilsung,Oh, Dong Young
, p. 4101 - 4105 (2007/10/03)
β-Amino phosphonate derivatives are synthesized in one-pot procedure via reduction of β-amino phosphonate intermediates with NaBH4/acetic acid or trifluoroacetic acid.