- A diversity of alkylation/acylation products of uracil and its derivatives: Synthesis and a structural study
-
tert-Butyl dicarbonate (Boc2O) and ethyl iodide (EtI) reactions with uracil (U), thymine (T) and 6-methyluracil (6-MU) were performed following routine procedures in pyridine/DMF solvents and with DMAP as the catalyst. Among 20 synthesized compounds, a derivative of 6-methyluracil substituted by the Boc-pyridine moiety at the C5 position appeared unexpectedly. The NMR spectra confirmed the molecular structure of all uracil derivatives. Parallel quantum mechanical DFT calculations supported the experimental findings.
- Michalak, Olga,Cmoch, Piotr,Krzeczyński, Piotr,Cybulski, Marcin,Le?, Andrzej
-
p. 354 - 362
(2019/01/10)
-
- A2B ADENOSINE RECEPTOR ANTAGONISTS
-
Disclosed are novel compounds that are A2B adenosine receptor antagonists having the following structure (I) wherein R1 and R2 are independently chosen from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl, and R4 is an optionally substituted heteroaryl moiety. The compounds of the invention are useful for treating various disease states, including asthma, chronic obstructive pulmonary disorder, pulmonary inflammation, emphysema, diabetic disorders, inflammatory gastrointestinal tract disorders, immunological/inflammatory disorders, cardiovascular diseases, neurological disorders, and diseases related to angiogenesis.
- -
-
Page/Page column 34
(2008/06/13)
-
- HSAB driven chemoselectivity in alkylation of uracil derivatives. A high yielding preparation of 3-alkylated and unsymmetrically 1,3-dialkylated uracils
-
A qualitative hardness scale (N134) has been found for the conjugated bases of 2-methoxy-4(3H)-pyrimidinones 1-3 and applied to high yielding chemoselective N3 methylation, ethylation and benzylation reactions. Removal of the 2-methoxy group followed by a second alkylation affords unsymmetrically 1,3-disubstituted uracils.
- Gambacorta, Augusto,Farah, Mohamed Elmi,Tofani, Daniela
-
p. 12615 - 12628
(2007/10/03)
-