Ethyl Acetate → Benzyl N-[(1S)-2-[(1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl]-1-(3-hydroxyadamantan-1-yl)-2-oxo ethyl]carbamate

関与物質

反応条件

反応手順

(2S)-2-{[(Benzyloxy)carbonyl]amino}-2-(3-hydroxyadamantan-1-yl)acetic acid of formula-XIV (20 gm), (1S,3S,5S)-2-azabicyclo[3.1.0]hexane-3-carbonitrile PTSA salt of Formula-XIII (16 gm), 1-ethyl-3-(3-dimethylaminoporpyl)carbodiimide (12 gm) and 1-hydroxy benzotriazole (1.2 gm) were dissolved in ethyl acetate (20 ml) and acetonitrile (40 ml). The reaction mixture was cooled to 20° C. Then addition of N,N-diisopropylethylamine (16 gm) was carried out for 15 min. The reaction mixture was stirred for 8 hrs and washed with 2N HCl solution. Organic phase was washed with NaHCO3 solution, dried and evaporated to yield 19.8 gm (80%) of title product. MP: 105-106° C.

情報源と証拠