CAS: 85293-16-9; 2-(2-(Piperazin-1-yl)Ethoxy)Ethan-1-Ol Dihydrochloride

相似化合物

13349-82-1 13349-82-1 68465-66-7

专利信息

专利号:WO-2008152434-A1
优先权日:2007-06-12
标 题 :Synthesis for the preparation of quetiapine
发明人：CZIBULA LASZLO; DOBAY LASZLO; FEHER KRISZTINA; WERKNE PAPP EVA
权利人:RICHTER GEDEON NYRT; CZIBULA LASZLO; DOBAY LASZLO; FEHER KRISZTINA; WERKNE PAPP EVA
摘要:Process for the synthesis of 2-[2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-piperazine-1-yl)-ethoxy]-ethanol of formula (I) (quetiapine) by reacting the 1-oxodibenzo-[b,f][1,4]thiazepine of formula (II) with phosphorus oxychloride by d) using 1-6 molequivalent of phosphorus oxychloride in an inert solvent and the obtained 11-chlorodibenzo[b,f][1,4]thiazepine compound of formula (IV) without isolation; e) is reacted further in an inert solvent in the presence of a base with 2-[2-(1-piperazinyl)-ethoxy]-ethanol dihydrochloride of formula (III a) or dihydrochloride monohydrate of formula (III b), in the mixture of an inert non-polar and dipolar aprotic solvent; f) in desired case the isolated quetiapine base of formula (I) is reacted with fumaric acid to form the hemifumarate salt thereof.