- PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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- Development of a Scalable Synthesis of 4-Aminopyrimidin-5-ol, a Versatile Intermediate
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A robust process for the preparation of multigram quantities of 4-aminopyrimidin-5-ol (5) in good yield from an inexpensive and readily available pyrimidine starting material is described. An initial evaluation of the reported literature route for this material utilizing a de novo pyrimidine synthesis provided safety concerns over the scalability of several intermediates. In addition, a number of steps proceeded in mediocre yield, and involved chromatographic separations for the desired products. The newly developed route mitigates the safety concerns, reduces the number of steps from five to three, avoids column chromatography, leads to an 8-fold improvement in yield, and utilizes reagents, which are recognized to be more environmentally benign.
- Le, Phuong T.,Richardson, Paul F.,Sach, Neal W.,Xin, Shuibo,Ren, Shijian,Xiao, Jiezhan,Xue, Liangliang
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p. 639 - 645
(2015/06/30)
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- Chiral 3-(4,5-dihydrooxazol-2-yl)phenyl alkylcarbamates as novel FAAH inhibitors: Insight into FAAH enantioselectivity by molecular docking and interaction fields
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Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are the main enzymes responsible for the hydrolysis of endogenous cannabinoids N-arachidonoylethanolamide (AEA) and 2-arachidonoylglycerol (2-AG), respectively. Phenyl alkylcarbamates are FA
- Myllymaeki, Mikko J.,Kaesnaenen, Heikki,Kataja, Antti O.,Lahtela-Kakkonen, Maija,Saario, Susanna M.,Poso, Antti,Koskinen, Ari M.P.
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experimental part
p. 4179 - 4191
(2009/12/04)
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- A new route to aminodiazines via metalation reaction. Synthesis of an aza analogue of Nevirapine: Diazines XV
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A new route to aminodiazines is reported, the ortho-directed lithiation of diazines is used, followed by reaction with tosyl azide as an electrophile. The reduction of the azido or tetrazolo compounds obtained was achieved and led to the expected amines. This methodology has allowed the synthesis of new aminodiazines and an improvement in the yield of various aminodiazines previously described. This reaction was used for the preparation of an aza analogue of Nevirapine.
- Plé, Nelly,Turck, Alain,Couture, Karine,Quéguiner, Guy
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p. 838 - 842
(2007/10/03)
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