IMPROVED METHOD FOR SYNTHESIS OF BETA-BLOCKER Russian patent published in 2011 - IPC C07C233/10 C07C231/12 

Abstract RU 2423346 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to a novel, improved method for synthesis of atenolol, comprising the following steps: a) a combination of chloromethylbenzene (XX) with isopropylamine to form N-benzyl-N-isopropylamine (XXII); b) reaction of the obtained N-benzyl-N-isopropylamine with epichlorohydrin (IIIA); c) conversion of halohydrin (XXIII-A) obtained at step b) in the presence of a base to epoxide; d) reaction of a phenylacetamide salt (XXV) with the halohydrin (XXIII-A) or epoxide (XXIV-A) in the presence of a base; e) debenzylation of the N-benzylated atenolol (XXVI-A) to racemic atenolol (I-A).

EFFECT: possibility of obtaining atenolol of high purity on an industrial scale.

11 cl, 24 ex

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RU 2 423 346 C2

Authors

Gkharpure Milind Moreshvar

Bkhaval Baburao Manikrao

Sutar Radzhiv Pandurang

Mekhta Satish Ramanlal

Dates

2011-07-10Published

2006-11-03Filed