FIELD: chemistry.
SUBSTANCE: present invention relates to a method of producing (E)-4-(6,7-dimethoxy-2-methyl-3-quinolyl)-3-buten-2-one derivatives of formula I, where Ia: R1 and R2 - CH3; Ib: R1 - CH3, R2 - C6H5; Ic: R1 - CH3, R2 - o-NO2C6H4; Id: R1 - t-Bu, R2 - C6H5; Ie: R1 - t-Bu, R2 - p-OCH3C6H4; If: R1 - p-BrC6H4, R2 - Ph; Ig: R1 -CH3, R2 - thiophene; Ih: R1 - t-Bu, R2 - CH2CH2Ph; Ii: R1 - t-Bu, R2 - CH2CH2Cl; Ij: R1 - p-BrC6H4, characterised by that ortho-aminoacylbenzylfuran derivatives of formula II are boiled in benzene in the presence of phosphorus oxychloride with a reflux condenser for 1.5-3.5 hours depending on substitutes R1 and R2.
EFFECT: obtaining (E)-4-(6,7-dimethoxy-2-methyl-3-quinolyl)-3-buten-2-one derivatives, pitavastatin analogues, and introduction of the required substitute into the desired compound with simultaneous formation of a quinoline nucleus.
2 tbl, 6 ex
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Authors
Dates
2011-07-27—Published
2010-01-11—Filed