PURPOSE: To obtain the heading compound which is an intermediate in the synthesis of a compound useful as an antihistaminic agent, etc., etc., simply and advantageously without by-products by contacting a specified amino acid with a Grignard reagent in a nonprotonic inactive organic solvent at a specified temperature.
CONSTITUTION: A free acid of formula I (R, an alkyl part of it is 1-6 C linear or branched and amino group NHR3 is bonded to one C of the alkyl part, is amino-substituted alkyl; R3 is H, 1-6 C linear or branched alkyl, benzyl, phenylethyl, 1-6 C linear or branched alkylene in which N is bonded to one C of the first alkyl part to form 5-8-membered N-containing saturated heterocycle) is contacted with a Grignard reagent of formula II (R1 and R2 are each H, 1-4 C alkyl, etc.; X is chloro, etc.) in a nonprotonic inactive organic solvent at a temperature between 20°C and the boiling point of the reaction mixture to obtain a compound of formula III.
| JPS5665847A | 1981-06-03 |