Method for obtaining pioglitazone as an antidiabetic agent

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

active

07009057

ABSTRACT:
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 —NHR3, wherein R3is hydrogen or a protecting group, which is removed before further treatment, and a residue of general formula (A), wherein Rbrepresents 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 Rbis 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)

REFERENCES:
patent: 2001/0008898 (2001-07-01), Tomiyama et al.
patent: 0 067 718 (1982-12-01), None
patent: 0 193 256 (1986-09-01), None
patent: 0 816 340 (1998-01-01), None
patent: 62 205054 (1987-09-01), None

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