Zentiva, A.s.

Zentiva K.s.

Ales Halama

Jindrich Richter

Josef Jirman

Ondrej Dammer

Petr Lustig

Stanislav Radl

Michal Voslar

Ludmila Hejtmánková

Lucie Srsnová

Pavel Zvatora

Ondrej Pisa

Kristyna Benediktova

Michal Zapadlo

Josef Cerny

A method for obtaining antidiabetic of formula (I), wherein the method comprises condensing of a 4-derivatized phenol or phenolate of general formula (II), wherein R is an amino group-containing organic residue, selected from the group comprising a residue of the following formula &#x2014;NHR, wherein Ris hydrogen or a protecting group, which is removed before further treatment, and a residue of general formula (A), wherein Rrepresents a carboxy group either in the free acid form or in the form of a salt or ester or another functional derivative or the nitrile group CN, and M represents a hydrogen or alkali metal atom, with a pyridine base of general formula (III, wherein Z is a leaving group other than a halogen, wherein, before or after carrying out the condensation, the following operations are carried out: (a) diazotizing the amino group present in organic residue R; (b) converting the diazotised residue R into a derivative of 2-halopropionate or 2-halopropionitrile of formula (B), wherein Ris as defined above and X is a halogen; (c) cyclizing the derivative of 2-halopropionate or 2-halopropionitrile with thiourea; (d) hydrolysing the resulting imine thus giving pioglitazone of formula (I)

Method for obtaining pioglitazone as an antidiabetic agent

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Pardubice, Czechia

Ales Halama