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To a solution comprising 5.97 g 2-(2,2-dimethoxyethylamino)pyridine (prepared as described by I. Kaye, in J. Am. Chem. Soc., 73, 5467 (195 1)) in 40 mL tetrahydrofurane, stirred under a nitrogen atmosphere at 0° C., was added, in a dropwise manner, 13.1 mL butyl lithium (2.5 M, in hexane). This was followed by removal of the cooling bath, and stirring of the obtained mixture for 1 h, at room temperature. There was then added, in a dropwise manner, 4.46 mL cyclohexanecarbonyl chloride. Then, after 5.5 h stirring at room temperature, 2 mL methanol was added. The solution was then evaporated to dryness under a vacuum, yielding a chestnut-colored oil; this product was then purified by flash chromatography (chloroform—ethyl acetate 7:3). The fractions containing the product were evaporated to dryness affording 8.3 g of Compound 1A (yield 78%); this substance was suitable for use in subsequent reactions with no additional purification processing.

1. customThis was followed by removal of the cooling bath
2. stirringstirring of the obtained mixture for 1 h, at room temperature
3. additionThere was then added, in a dropwise manner, 4.46 mL cyclohexanecarbonyl chloride
4. stirringThen, after 5.5 h stirring at room temperature
5. addition2 mL methanol was added
6. customThe solution was then evaporated to dryness under a vacuum
7. customyielding a chestnut-colored oil
8. customthis product was then purified by flash chromatography (chloroform—ethyl acetate 7:3)
9. additionThe fractions containing the product
10. customwere evaporated to dryness