SYNTHESIS OF 3-AMINO-3-ARYLPROPANOATES Russian patent published in 2004 - IPC

Abstract RU 2225859 C2

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to the improved method for preparing compound of the formula (I): wherein R1 represents aryl, heteroaryl, substituted aryl or substituted heteroaryl; R2 represents hydrogen atom, alkyl or aralkyl; or its salts. Method for preparing involves interaction of compound of the formula (II): wherein R1 such as described above; R2′ represents alkyl or aralkyl with compound of the formula (III): wherein R5 represents hydrogen atom or alkoxy-group under reduced pressure, at boiling temperature of reaction solution (from 40 C to 65 C) in inert medium and with azeotropic water distilling off. The prepared compound of the formula (IV): is treated with gaseous hydrogen in the presence of palladium catalyst to obtain compound of the formula (V): that in interaction with acid converts to compound of the formula (I); or by interaction of compound of the formula (IV) with gaseous hydrogen in the presence of palladium catalyst and conversion of prepared compound of the formula (V) by treatment with acid to the end product; to intermediate compounds used for synthesis of compounds of the formula (I), new compounds of general formulas (IV) and (V). The proposed method can be used in large-scale manufacturing compounds of the formula (I) with acceptable purity and yield indices. EFFECT: improved preparing method. 22 cl, 3 ex

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RU 2 225 859 C2

Authors

Abdel'-Magid Akhmed F.

Kokhen Judit Kh.

Mar'Janoff Sintija A.

Villani Frehnk Dzhon Ml.

Zong Khua M.

Dates

2004-03-20Published

2000-03-21Filed