PURPOSE: To readily and efficiently obtain the subject compound in high purity and yield by reacting α-amino-α-methyl-β-dioxyphenyl-propionitriles and ketones as starting material, then hydrolyzing under specific condition.
CONSTITUTION: A compound of α-amino-α-methyl-β-dioxyphenyl-propionitriles expressed by formula I (R1 and R2 are H or lower alkyl) or formula II (n is 1-4) is reacted with ketones in organic solvent such as methanol and in the presence of strong basic substance such as NaOH at from -10 to 50°C, for 5-7 hour at about 10°C to obtain oxazolidine-type compound expressed by formula III (R3 and R4 are lower alkyl) or formula IV, then acidic substance such as hydrochloric acid is added to adjust to neutral or acidic, preferably pH6-7, hydrolyzed at 0-50°C for 1-5 hour, thus the aimed compound expressed by formula V or formula VI useful as raw material of α-methyl dopa as excellent remedy of essential hypertension is obtained.
| JPS5492937 | HYDROXYPHENYL ALANINE DERIVATIVE |
| JP2006519874 | Diphenylethylene compounds and their use |
HIGUCHI HIROBUMI
KONDO TOSHIO
UCHIYAMA TAKAKO
