- Safety evaluation of an unexpected incident with a nitro compound
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An unexpected highly exothermic reaction followed by explosion has been studied by means of reaction calorimetry and adiabatic calorimetry. The investigation of the process shows that the incident took place by a local adiabatic temperature rise in the reactor vessel due to the presence of potassium carbonate, which activated the decomposition of a nitro compound with an unusual low temperature onset The study is completed with an unproved and safer procedure consisting of changing the order of chemicals addition as an alternative approach.
- Barbas, Rafael,Botija, Manuel,Camps, Helena,Portell, Anna,Prohens, Rafel,Puigjaner, Cristina
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Read Online
- Design and synthesis of N-Aryl isothioureas as a novel class of gastric H+/K+-ATPase inhibitors
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To find new H+/K+-ATPase inhibitors for the treatment of peptic ulcer disease, a series of novel N-aryl isothiourea derivatives were synthesized and their structures were identified by 1H NMR and GC-MS. The effects of these compounds on inhibiting gastric acid secretion were evaluated by the guinea pig stomach mucous membrane study with pantoprazole magnesium as a positive control. The results showed that, of the 37 N-aryl isothiourea compounds synthesized, 20 compounds have comparable or stronger gastric acid inhibitory activities than that of pantoprazole magnesium. The quantitative structure-activity relationships (QSARs) of the N-aryl isothiourea compounds were also studied by comparative molecular field analysis (CoMFA) computation, and the model structure that was supposed to give more powerful bioactivities was finally predicted. A series of novel N-aryl isothiourea derivatives were synthesized and evaluated for their effects of inhibiting gastric acid secretion using the guinea pig stomach mucous membrane study with pantoprazole magnesium as a positive control. Compounds 2c, 2e, and 2k have higher bioactivity. The quantitative structure-activity relationships also defined these structural requirements.
- Ma, Chao,Wu, Anhui,Wu, Yongqi,Ren, Xuhong,Cheng, Maosheng
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p. 891 - 900
(2014/01/06)
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- Diversified synthesis of novel quinoline and dibenzo thiazepine derivatives using known active intermediates
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The novel drug development to control resisting infections in conventional drug therapy is a need of today. Few antiulcer relative derivatives developed by approaching convergent synthesis. The derivatives synthesized successfully are dibenzo thiazepine-pyridine (SLN11-SLN15) and benzimidazole-hydroquinoline based derivatives (SLN16-SLN20). It involved the coupling through microwave, sonication and conventional techniques at final step. The efficient technology identified as sonication technique basically time and yield. The reported compounds were structural characterized by elemental analysis and spectral studies such as 1H, 13C NMR and MS.
- Sharada,Satyanarayana Reddy,Sammaiah,Sumalatha
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p. 7959 - 7966
(2013/09/23)
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- Process for preparing lansoprazole
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The invention relates to a process for preparing lansoprazole. It is also directed to lansoprazole having a specific surface area and a pharmaceutical composition comprising lansoprazole.
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Page/Page column 8
(2008/06/13)
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- Crystals of benzimidazole derivatives and their production
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A substantially solvent-free and stable crystal of the compound of the formula: STR1 wherein the ring A may optionally be substituted, R1 represents hydrogen or an N-protecting group, each of R2, R3 and R4 (1) a hydrogen atom, (2) an alkyl group which may optionally be substituted with halogen atom(s) or (3) an alkoxy group which may optionally be substituted with halogen atom(s) or alkoxy; or its salt, is produced by subjecting a solvate of the compound (I) or its salt to de-solvent treatment, in an industrially advantageous method.
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- Method of producing nitrogen-containing heteroaromatic compounds having an alkoxy group
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Nitrogen-containing heteroaromatic compounds having an alkoxy group can be produced by reacting nitrogen-containing heteroaromatic compounds having a nitro group with alcohol or alcoholate in the presence of a phase transfer catalyst and a base.
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