专利号:US-8389716-B2 优先权日:2009-01-30 标题:Process for the synthesis of quetiapine 发明人:SERAFINI SIRO; TOMASI FILIPPO; GALVAGNI MARCO 权利人:SERAFINI SIRO; TOMASI FILIPPO; GALVAGNI MARCO; ITALIANA SINT SPA 摘要:The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base.
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.
专利号:US-9304126-B2 优先权日:2012-08-21 标题:Haptens of quetiapine 发明人:DONAHUE MATTHEW GARRETT; GONG YONG; SALTER RHYS; HRYHORENKO ERIC; DECORY THOMAS R; REMMERIE BART; SANKARAN BANUMATHI 权利人:JANSSEN PHARMACEUTICA NV; ORTHO CLINICAL DIAGNOSTICS INC 摘要:The invention relates to compounds of Formula I, wherein R 1 , R 2 , and R 3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from quetiapine. The invention also relates to conjugates of a quetiapine hapten and a protein.
专利号:EP-0844261-A1 优先权日:1996-11-21 标题:Dispersions containing polyurethanes with carbonyl groups in ketone function 发明人:KOKEL NICOLAS DR; GULBINS ERICH DR; RAU MARIA GYOPAR DR; FISCHER GERHARD 权利人:BASF AG 摘要:R 1 , R 2 , R 3 jeweils Wasserstoff, C 1 - bis C 24 -Alkyl oder C 6 - bisnC 24 -Alkenyl R 4 Wasserstoff R 5 , R 6 a) gemeinsam C 4 - bis C 10 -Alkandiyl, b) jeweils C 2 - bis C 10 -Alkyl, C 5 - bis C 8 -Cycloalkylnoder C 7 - bis C 20 -Aralkyl, c) jeweils ein hydroxylterminiertes Poly-(C 2 - bisnC 4 -alkylenoxid), oder d) ein Rest R 5 oder R 6 die unter (a) bis (c) angegebenenBedeutung und der andere Rest Wasserstoffnoder ein Rest der Formel IIn nin der X C 2 - bis C 6 -Alkandiyl bedeutet und R 7 gleichbedeutend ist mit R 5 oder R 6 mit der Ausnahme,ndaß R 7 nicht ein Rest der Formel II bedeutet, nwobei n die Reste R 5 und R 6 in jedem der Fälle (a) bis (d) insgesamtneine (1) an ein aliphatisches C-Atom gebundene Hydroxylgruppenntragen, gegebenenfalls der Rest R 5 und/oder R 6 1 oder 2 aromatischngebundene Hydroxylgruppen oder 1 Nitril-, tertiäre Amino-,nCarbonsäure- oder Sulfonsäuregruppe, die gegebenenfalls innForm ihrer Salze vorliegen, trägt, und die mittlere Funktionalität (F) aller Aufbaukomponenten desnPolyurethans (A), bezogen auf die Funktionalitäten, die beimnAufbau des Polyurethans (A) in einer Additionsreaktion miteinandernreagieren, 1,5 bis 2,2 beträgt. Aqueous dispersions containing a polyurethane (A) with structural units which differ from compounds of the formula (I) in which the substituents have the following meaning: R 1 , R 2 , R 3 in each case hydrogen, C 1 - to C 24 -alkyl or C 6 - to C 24 -alkenyl R 4 hydrogen R 5 , R 6 a) together C 4 - to C 10 -alkanediyl, b) in each case C 2 to C 10 alkyl, C 5 to C 8 cycloalkyl or C 7 to C 20 aralkyl, c) in each case a hydroxyl-terminated poly (C 2 - to C 4 -alkylene oxide), or d) a radical R 5 or R 6 has the meaning given under (a) to (c) and the other radical is hydrogen or a radical of the formula II in the X C 2 - to C 6 -alkanediyl means and R 7 is equivalent to R 5 or R 6 with the exception that R 7 does not represent a radical of the formula II, in which the radicals R 5 and R 6 in each of cases (a) to (d) carry a total of one (1) hydroxyl groups bonded to an aliphatic carbon atom, optionally the radical R 5 and / or R 6 carries 1 or 2 aromatically bound hydroxyl groups or 1 nitrile, tertiary amino, carboxylic acid or sulfonic acid group, which are optionally present in the form of their salts, and the average functionality (F) of all structural components of the polyurethane (A), based on the functionalities which react with one another during the synthesis of the polyurethane (A) in an addition reaction, is 1.5 to 2.2.
专利号:US-8053165-B2 优先权日:2008-03-18 标 题:Hydroxyl-containing monomer, polymer, resist composition, and patterning process 发明人:KINSHO TAKESHI; OHASHI MASAKI; HASEGAWA KOJI; WATANABE TAKERU 权利人:SHINETSU CHEMICAL CO 摘要:A hydroxyl-containing monomer of formula (1) is provided wherein R 1 is H, F, methyl or trifluoromethyl, R 2 and R 3 are monovalent C 1 -C 15 hydrocarbon groups, or R 2 and R 3 may form an aliphatic ring. The monomers are useful for the synthesis of polymers which have high transparency to radiation of up to 500 nm and the effect of controlling acid diffusion so that the polymers may be used as a base resin to formulate radiation-sensitive resist compositions having a high resolution.
专利号:US-2011118460-A1 优先权日:2009-01-30 标 题:Process for the synthesis of quetiapine
参考文献:10.1186/s13065-016-0231-7 摘要:Saeed IM, Lee VS, Mazari SA, Si Ali B, Basirun WJ, Asghar A, Ghalib L, Jan BM. Thermal degradation of aqueous 2-aminoethylethanolamine in CO2 capture; identification of degradation products, reaction mechanisms and computational studies. Chemistry Central Journal. 2017 Jan 24;11(1). doi: 10.1186/s13065-016-0231-7. 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003). 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).