METHODS OF PRODUCING SOME 2-(PYRIDIN-3-YL)THIAZOLES Russian patent published in 2018 - IPC C07D417/04 C07D213/83 

FIELD: chemical industry.

SUBSTANCE: invention relates to a method of producing 2-(pyridin-3-yl)thiazoles of formula (IV), where (A) each R¹ is H; (B) R² is (C₁-C₆) alkyl; (C) R³ is H and (D) R⁴ is (C₁-C₆) alkyl. Method is implemented by (i) reacting compound (I) with compound (IIa) to form compound (IIb), wherein the said reaction is carried out at the ambient temperature and at the ambient pressure in a polar protic solvent; (ii) reacting compound (IIb) with compound (IIc) to form compound (III), wherein the said reaction is carried out at the ambient temperature and at the ambient pressure in a polar solvent; and (iii) cyclizing compound (III) using a dehydrating reagent to form compound (IV), wherein the said reaction is carried out at the ambient temperature and at the ambient pressure in a polar aprotic solvent. Said polar protic solvent of stage a1 is formic acid, n-butanol, isopropanol, n-propanol, ethanol, methanol, acetic acid, water or a mixture thereof. On stage b compound (III) is cyclized using a dehydrating reagent selected from POCl₃, H₂SO₄, SOCl₂, P₂O₅, polyphosphoric acid, p-toluenesulfonic acid, trifluoroacetic anhydride or a mixture thereof. Method further comprises halogenating said R³ up to F, Cl, Br or I.

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EFFECT: technical result is a method of producing 2-(pyridin-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazolamides.

11 cl, 2 ex