Hydrochloric Acid → 6-(aminomethyl)-3-(3,4-dimethoxybenzyl)-1-(tetrahydro-2H-pyran-4-yl)quinazoline-2,4(1H,3H)-dione

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Reaction Steps

A mixture of 0.55 g of the compound obtained in Step 12.1, and 2.94 ml of a 2M borane/dimethyl sulfide complex in THF, in 15 ml of THF is irradiated in a microwave field for 1 minute at 100° C. The reaction medium is taken up in DCM. 50 ml of 1N HCl are added and the mixture is stirred for 2 hours at room temperature. The resulting mixture is neutralized with 2N sodium hydroxide solution. This resulting mixture is extracted with DCM, dried over Na2SO4, filtered and evaporated under reduced pressure. The residue is chromatographed on an RP18 column, eluting with a water/ACN mixture from (90/10, v/v) to (50/50, v/v) to give 0.23 g of the expected product.

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