PURPOSE: To prepare 3-N-substituted carbamoylthiopropionic acid derivative having analgesic, antiphlogistic and immuno-regulating activities, in one step and in high yield, from a low-cost, non-toxic thiocarbamic acid derivative and a propionic acid derivative.
CONSTITUTION: The titled compound IV is prepared by reacting a thiocarbamic acid derivative I (R1, R2 are H, lower alkyl, aralkyl, aryl, or form together with adjacent N atom a heterocyclic ring) with a propionic acid derivative II (R3, R4 are H, lower alkyl, aralkyl or aryl) or III (Y is halogen). The reaction is pref. carried out in an inert solvent, at room temp., or if necessary with heating or cooling, in the presence of a basic catalyst.
USE: The compound IV is also useful as an intermediate of the compound V which is an effective hypotensor.
SHIRAKI MASAKI
ABE YUKIO
