METHOD FOR PREPARING QUETIAPINE AND INTERMEDIATE COMPOUNDS Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine.

SUBSTANCE: invention describes a method for preparing 11-{4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl}-dibenzo[b,f]-1,4-thiazepine of the formula (I): or its pharmaceutically acceptable additive acid salt. Method involves: (a₁) interaction of halogenethylpiperazinylthiazepine derivative of the formula (VIII): wherein Hal means halogen atom with ethylene glycol; or (a₂) cyclization reaction of halogenethylpiperazine derivative of the formula (VII): wherein Hal represents halogen atom in the presence of dehydrating agent and interaction of synthesized derivative of halogenethylpiperazinylthiazepine of the formula (VIII) wherein Hal is given above with ethylene glycol; or (a₃ interaction of hydroxyethylpiperazine derivative of the formula (VI): with halogenating agent, cyclization reaction of synthesized derivative of halogenethylpiperazine of the formula (VII) wherein Hal means halogen atom in the presence of dehydrating agent and interaction of synthesized derivative of halogenethylpiperazinylthiazepine of the formula (VIII) wherein Hal is given above with ethylene glycol; or (a₄) interaction of hydroxyethylpiperazine derivative of the formula (VI) with halogenating agent and dehydrating agent simultaneously and interaction of synthesized derivative of halogenethylpiperazinylthiazepine of the formula (VIII) wherein Hal means halogen atom with ethylene glycol; or (a₅) interaction of urethane derivative of the formula (IV): with 1-(2-hydroxyethyl)-piperazine of the formula: and the following interaction of formed hydroxyethylpiperazine of the formula (VI) with halogenating agent and dehydrating agent and interaction of synthesized derivative of halogenethylpiperazinylthiazepine of the formula (VIII) wherein Has means halogen atom with ethylene glycol; and, if necessary, conversion of synthesized product to acid additive salt to form pharmaceutically acceptable inorganic or organic acid. Also, invention describes a derivative of piperazine of the formula (IX) given in the invention description. Invention provides the development of economic method for preparing quethiapine.

EFFECT: improved preparing method.

10 cl, 4 ex