(R)-色满-2-基甲胺盐酸盐

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: 20.3 g of (R)-2-aminomethylchroman hydrochloride are introduced into 150 ml of ethanol, and 36.8 g of a 20% solution of sodium ethoxide in ethanol are added dropwise with stirring. 20.5 g of 5-(4-fluorophenyl)pyridine-3-carbaldehyde are added to the suspension at 35° C., and the mixture is stirred for a further 3 hours. After addition of 4.2 g of sodium borohydride, the mixture is stirred for a further 4 hours, and 62 ml of water are then added dropwise at room temperature. The pH of the reaction mixture is then adjusted to pH 4 using 37% hydrochloric acid over the course of one hour. The crystals are filtered off, rinsed with ethanol and dried under reduced pressure, giving 27.2 g of (R)-(−)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman hydrochloride (69% yield). are added dropwise the mixture is stirred for a further 3 hours the mixture is stirred for a further 4 hours over the course of one hour The crystals are filtered off rinsed with ethanol dried under reduced pressure

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: According to the method of Example 160, 2-cyano-2-(3,4-dichloro-5-oxo-2,5-dihydrofuran-2-yl)acetamide was reacted with 1-[(2R)-3,4-dihydro-2H-chromen-2-yl]methanamine hydrochloride to give the title compound.