Oxidative process and products thereof
AssigneeJanssen Pharmaceutica NV
InventorsJames Henshilwood, Nicholas Bernard Johnson
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Abstract
The subject invention concerns a process for the preparation of a compound of formula (2), which comprises phenolic oxidation of a compound of formula (1) wherein X1 and X2 are independently selected from H or a protecting group for the phenolic function, e.g. acyl or trialkylsilyl; groups A1, A2, B1, B2 and Y are selected so as to render the nitrogen atom non-basic; Z is a blocking group, e.g. Br or t-butyl; and R is H, alkyl, aryl, or arylalkyl, and wherein the process is carried out in a two-phase liquid system comprising an aqueous base and an organic solvent having a dielectric constant below 4.8.
Claims10
A process for the preparation of a compound of formula (2), comprising phenolic oxidation of a compound of formula (1)
- wherein X1 and X2 are independently selected from H or a protecting group for the phenolic function;
- groups A1, A2, B1, B2 and Y are selected from the group consisting of (i) wherein each of A1, A2, B1 and B2 are H and Y is COR1, wherein R1 is selected from the group consisting of H, alkyl, aryl, arylalkyl, and alkyloxy;
- (ii) wherein A1 and A2 are H, B1 and B2 are, together, O, and Y is H or Me;
- and (iii) wherein A1 and A2 are, together, O, B1 and B2 are H, and Y is H or Me;
- Z is a blocking group;
- and R is selected from the group consisting of H, alkyl, aryl, and arylalkyl, and wherein the process is carried out in a two phase liquid system comprising an aqueous base and an organic solvent having a dielectric constant below 4.8, as measured at 20° C., wherein said solvent is toluene.
Dependencies are inferred from the claim text.