专利号:US-4532322-A 优先权日:1983-05-23 标题:Preparation of thiazine derivatives 发明人:JACKSON ARTHUR; HEYES GRAHAM 权利人:FINE ORGANICS LTD 摘要:A method for the preparation of a thiazine derivative of the formula ##STR1## where each R is independently selected from hydrogen or a lower alkyl having 1 to 4 carbon atoms, the method comprising reacting together a sulphur donor which is selected from sulfur, ammonium or alkali metal sulfides, ammonium or alkali metal hydrosulfides, or hydrogen sulfide, 1,1-bis(methylthio)-2-nitroethene and a compound of the formula n n H.sub.2 NCR.sub.2 CR.sub.2 CR.sub.2 OSO.sub.3 H n n where each R is as defined above. n A preferred method is for the preparation of tetra-2-(nitromethylene)-2H-1,3-thiazine which possesses broad spectrum insecticidal activity, and is also useful as an intermediate in the synthesis of other insecticides.
专利号:US-4967007-A 优先权日:1989-05-10 标 题 :Improved process for the preparation of 1-substituted amino-1-substituted thio-2-nitro alkenes 发明人:DESHMUKH ABDUL R A S; BHAWAL BABURAO M; SHIRALKAR VASUDEO P; RAJAPPA SRINIVASACHARI 权利人:COUNCIL SCIENT IND RES 摘要:A process is disclosed for the manufacture of 1-substituted amino-1-substituted thio-2 nitro alkenes of the general formula: (R1NH) (R2S) Câ•?CR3 (NO2) wherein R1, R2, R3, may be same or different and may consist of hydrogen, alkyl, aryl or arylalkyl groups or combinations thereof. These alkenes are prepared by reacting a primary amine with a compound of sulfur in the presence of a primary catalyst to obtain a carbonimidodithioic acid salt which is converted to a corresponding ester which is thereafter reacted with a nitro compound in the presence of a secondary catalyst. 1-methylamino-1-methylthio-2-nitroethene is an important intermediate in the synthesis of Rantitidine and Nizatidine which are used as effective drugs in the treatment of peptic ulcers and associated gastrointestinal disorders.
专利号:RU-2042671-C1 优先权日:1990-11-09 标 题:Diketoneimine derivative as an intermediate product for synthesis of ranitidine and method of its synthesis
专利号:WO-0029400-A2 优先权日:1998-11-19 标 题 :Procedure for synthesis of n-[2[[[5- [(dialkilamino) methyl]-2- furanyl] methyl]thyo] ethyl]-n'- alkyl-2-nitro1,1 alkenediamines and their hydrochlorides
专利号:EP-0486461-B1 优先权日:1990-11-09 标 题:A diketene imine derivative and process for preparing same 发明人:JESZENSKI ANDOR DIPL-CHEM; LOSONCZI BELA DR DIPL-CHEM; CZEH MARIA; GODO LASZLO; STEFKO BELA DR; BENCZIK TAMAS DIPL-CHEM ING; HERMANN LAZSLO DIPL-CHEM ING; HAVASI GABOR DIPL-CHEM ING; KALVIN PETER DIPL-CHEM ING; STEFAN LASZLO DIPL-CHEM ING; MEGYERI GABOR DR DIPL-CHEM ING 权利人:RICHTER GEDEON VEGYESZET 摘要:The invention relates to the novel compound of formula (I), chemically 1-{2-[(5-N,N-dimethylaminomethyl-2-furyl)-methylthio]ethyl}-2-{2-[(5-N ,N-dimethylaminomethyl-2-furyl)-methylthio]-1-ethylamino} -3-nitro-4-nitromethylene-2-azetine, which is a useful key intermediate in the synthesis of 1-{2-[(5-dimethylaminomethyl-2-furyl)methylthio]ethyl}-amino-1-methyla mino-2-nitroethylene (generic name: ranitidine), a known H-2 receptor antagonist. The invention further relates to a process for the preparation of the compound of formula (I), which can be carried out in one simple process step on industrial scale, too. The compound of formula (I) can easily be transformed to ranitidine in one simple step.
专利号:US-4777260-A 优先权日:1985-12-18 标题 :Synthesis of nizatidine intermediate 发明人:RYAN CHARLES W; SLOMSKI BRUCE A 权利人:LILLY CO ELI 摘要:The present invention provides a process for preparing a novel intermediate for nizatidine.
[参考文献]: Nasrin Zohreh, Et Al. Uncatalyzed One-Pot Synthesis Of Highly Substituted Pyridazines And Pyrazoline-Spirooxindoles Via Domino Sn/condensation/aza-Ene Addition Cyclization Reaction Sequence. Acs Comb Sci. 2013 Jun 10;15(6):278-86.
合成参考文献
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 120. 摘要:Liu, Q., Science of Synthesis Knowledge Updates, (2014) 2, 274.