Process for preparing achpa

Details Process for preparing achpa Process for preparing achpa

C - Chemistry, Metallurgy

07

C

260/469

C07C 269/06 (2006.01) C07C 271/06 (2006.01) C07C 271/22 (2006.01)

Patent

CA 1313881

5835P/1200A 17608 TITLE OF THE INVENTION: IMPROVED PROCESS FOR PREPARING ACHPA ABSTRACT OF THE DISCLOSURE A process for preparing (3S,4S)-N-.alpha.-BOC)-4- amino-5-cyclohexyl-3-hydroxypentanoic acid ethyl ester comprising (a) reacting the N-.alpha.-BOC-amino-3- hexahydrophenyl propionic acid with 1,1- carbonyldiimidazole, to form an acylimidazol-activated derivative of said acid; (b) coupling said acylimidazole- activated derivative with the magnesium salt of malonic acid monoethylester to afford the .beta.-ketoester; (c) reducing said .beta.-ketoester using sodium cyanoborohydride in tetrahydrofuran and glacial acetic acid to produce a mixture of (3S,4S)-(N.alpha.-BOC)-4-amino-5- cyclohexyl-3-hydroxypentanoic acid ethyl ester and (3B,4S)-(N.alpha.-BOC)-4-amino-5-cyclohexyl-3-hydroxypentanoic acid ethyl ester; (d) crystallizing off the (3R,4S) compound and purifying the remaining product to afford optically-pure (3S,4S)-(N.alpha.-BOC)-4-amino-5-cyclohexyl-3- hydroxypentanoic acid.

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