engleski

Kinetic Resolution of Diastereomeric Racemates of 7-Bromo-3-(1`-hydroxy-ethyl)-1-methyl-5-(2`-pyridyl)-2, 3-dihydro-1H-1, 4-benzodiazepin-2-one by Immobilized CAL-B

Immobilized CAL-B catalyzed kinetic resolution of syn-7-bromo-3-(1`-hydroxy-ethyl)-1-methyl-5-(2`-pyridyl)-2, 3-dihydro-1H-1, 4-benzodiazepin-2-one syn-( )-2) and its anti-diastereomer ( )-3) are achieved with E-values over 200. Completely enantioselective acetylation of (1´R)-enantiomers in diastereomeric racemates with opposite configuration at the second stereogenic center C(3) occurs at substantially different rate (t1/2syn/t1/2anti ca 1/20). Conformational origins of enantioselection are discussed.

Kinetic Resolution; Diastereomeric Racemates

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