Isopropylamine → (S)-Metoprolol

Participants

Reaction Steps

171 mg of (+)-4-(2-methoxyethyl)-phenyl glycidyl ether were reacted with isopropylamine (method as in Example 2) to obtain 154 mg of (-)-metoprolol melting at 44-45° C. with [α]D25= - 5.27° (c =0.967 in ethanol). Optical purity was determined to be 98.4% based on HPLC of the S-leucyl diastereomeric derivatives as in Example 2. Evaporation of the mother liquor gave 6 mg of (-)-metoprolol of 92.2% optical purity.

Provenance & Evidence