(XII): where R1 and R2 are as defined in any one of claims 1 to 3 and Pg represents a protective group, is reacted with an amine of formula HNR8R9, in which R8 and R9 are as defined in any one of claims 1 to 5, and then in that the protective groups are removed from the ...
Such kind of substances normally need a certain amount of time to react with the enzyme and inactivate it. Allowing the compound to interact with the enzyme before adding the substrate consequently increases its inhibitory activity. However, the relatively weak inhibition in the assay without pre-...
In one embodiment, a compound of formula I wherein R6is NHC(NH)NH2, R7is methyl and R8is hydrogen may e.g. be treated with 3-dimethylamino-1-(3-pyridyl)-2-propen-1-one to a compound of formula IV wherein R6′ is 4-(3-pyridyl)-2-pyrimidinamino, R7′ is methyl and R8′ is h...
The compound is then reacted with an equimolar quantity to slight excess of the compound having the good leaving group. The reaction is conducted in a suitable aprotic solvent such as N,N-dimethylformamide, N,N-dimethylacetamide and related solvents. The reaction is substantially complete after ...
2. A process as claimed in claim 1, wherein the thien-(3)-yl lithium is reacted with the compound of formula (II) at a temperature below -70° C. 3. A process as claimed in claim 2, wherein the reaction of the thien-(3)-yl lithium with the compound of formula (II) is carri...
The synthesis method provided by the present invention thus makes it possible to obtain the alcohol (VI) from the dihydrocoumarin (II) with the same number of steps as in the prior art, but avoiding the use of reactants such as LiAlH4 or AlCl3, which are problematic to use given their...
The '203 process to convert CC to DD is complicated and carried out as a one pot reaction (Scheme 2). Applying the conditions of the '203 process, the nitro moiety of 3 (of the present invention) is reduced to the aniline derivative which then reacts with aldehyde 5 to form the ...