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:US-4761413-A 优先权日:1986-12-22 标 题:1,5-epoxy-2,3,4,5-tetrahydro-1H-3-benzazepins and use in treatment of ulcers 发明人:WACHTER MICHAEL P; KARANEWSKY DONALD S 权利人:ORTHO PHARMA CORP 摘要:The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.
专利号:US-4855426-A 优先权日:1986-12-22 标题:Process of preparing 1,5-epoxy-2,3,4,5-tetrahydro-1H-3-benzazepins 发明人:WACHTER MICHAEL P; KARANEWSKY DONALD S 权利人:ORTHO PHARMA CORP 摘要:The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.
专利号:US-5030738-A 优先权日:1986-03-28 标 题:Synthesis of antiulcer compounds 发明人:REINER ALBERTO 权利人:JANUS FARMA SRL 摘要:To synthesize molecules with antiulcer action, specifically ranitidine, niperotidine and cimetidine, having the formula: ##STR1## wherein R 1 is hydrogen or together with R 2 represents the rest of a cycloaliphatic or heterocyclic optionally substituted ring with 5 or 6 carbon atoms, R 2 represents H, alkyl, alkyl substituted with a simple or substituted aromatic ring or with a single or substituted heterocyclic ring, Ar represents a simple or substituted phenyl group, a simple or substituted heterocyclic aromatic group, N=1, 2, 3, 4, 5 or 6 and X represents CH--NO 2 , S, N--C.tbd.N, the compound (II) is prepared through the following process sequence: ##STR2## wherein Z=H, NO 2 , halogen and R 3 =--(CH 2 ) n Ar, --(CH 2 ) n --SH, --(CH 2 ) n --S--S--(CH 2 ) n , --(CH 2 ) n --S--CH 2 Ar Y being halogen. n The urea of formula ##STR3## is converted in a first stage into the corresponding carbodiimide ##STR4## by reaction with triphenylphosphine and bromine in the presence of a strong base and in a second stage is obtained the desired compound by reaction with nitromethane or with a saline derivative of cynamide.
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:US-4910198-A 优先权日:1986-12-22 标题:1,5-epoxy-2,3,4,5-tetrahydro-1H-3-benzazepins 发明人:WACHTER MICHAEL P; KARANEWSKY DONALD S 权利人:ORTHO PHARMA CORP 摘要:The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.