Alkoxylation of 2,3-dialkylindoles utilizing iodosobenzene diacetate

1980 ◽  
Vol 58 (15) ◽  
pp. 1589-1591 ◽  
Author(s):  
Dennis V. C. Awangz ◽  
André Vincent

Iodosobenzene diacetate has been employed in the development of a simple procedure for the production of 3-alkoxyindolenines from 2,3-disubstituted indoles, by treatment of the indoles with the reagent in alcoholic solvent.Primary and secondary alkoxy functions have been incorporated at the β-site of 2,3-dimethylindole but the reaction with tert-butanol leads to other complex products. Good yields of 9-n-alkoxy-9H-reserpines have been realised but no reaction is observed in secondary alcohols.

1979 ◽  
Vol 57 (20) ◽  
pp. 2727-2733 ◽  
Author(s):  
Lê H. Dao ◽  
Donald Mackay

Two equivalents of the title compound (1) react with one equivalent of primary alcohols to give good yields of nitrogen and 1-alkoxycarbonyl-2-N-phenylcarbamoyl-4-phenyl-1,2,4-triazolidine-3,5-di ones (3). With secondary alcohols or benzyl alcohol the major products are the ketone or benzaldehyde, while 3 are minor products. The latter can, however, be made the major products if pyridine is used to catalyze the reaction. Compound 3a dissociates on heating or in pyridine solution into the 1-methoxycarbonyltriazolidinedione 4.If alcohols are absent 1 is converted by pyridine or other tertiary amines into nitrogen and the bicyclic compound 9; if diethyl azodicarboxylate is present in the reaction compound 13 can be trapped.Primary and secondary amines react very rapidly with 1 to give nitrogen and complex products. It is likely that these are 1,2-dicarbamoyl-4-phenyltriazolidine diones, analogous to 3, and that they are very prone to dissociate in solution.


1997 ◽  
Vol 75 (5) ◽  
pp. 559-566 ◽  
Author(s):  
Yixing Zhao ◽  
Gordon R. Freeman

The electrical conductances of the small-ion salts LiI and LiNO3 in water and C1–C4 alcohols were measured at different temperatures. At the concentrations used, ion association was negligible except when εT < 4200 K, where ε is the relative permittivity of the solvent at temperature T. Consistent with Walden's rule, the values of ηΛ0 in each solvent are nearly constant as the temperature is increased; the value for LiI in each solvent is slightly higher than that for LiNO3. Ion association occurs in tert-butanol and is more extensive for LiNO3 than that for LiI; the planar NO3− ions fit less well than the spherical I− ions into the packing of the rigid, spherical tert-butanol molecules. The effective radius of solvated ions in CN primary alcohols increases approximately as the length of the randomly folded chain, (N + 1)1/2. For secondary alcohols this factor is somewhat too small for small-ions and too large for large tetraphenyl ions. The values of EΛ0 are close to the values of Eη in the corresponding alcohols. Keywords: electrical conductivity, large ions, small-ions, alcohols, solvent effects.


1995 ◽  
Vol 73 (03) ◽  
pp. 535-542 ◽  
Author(s):  
N Crawford ◽  
A Chajara ◽  
G Pfliegler ◽  
B EI Gamal ◽  
L Brewer ◽  
...  

SummaryDrugs can be electro-encapsulated within platelets and targeted to damaged blood vessels by exploiting the platelet’s natural haemostatic properties to adhere to collagen and other vessel wall constituents revealed by injury. A rat aorta balloon angioplasty model has been used to study the effect on platelet deposition of giving iloprost loaded platelets i.v. during the balloon injury. After labelling the circulating platelets with 111-Indium before balloon injury, time course studies showed maximum platelet deposition on the injured aorta occurred at about 1 h post-injury and the deposition remained stable over the next 2-3 h. When iloprost-loaded platelets were given i.v. during injury and the circulating platelet pool labelled with 111-Indium 30 min later, platelet deposition, measured at 2 h postinjury, was substantially and significantly reduced compared with control platelet treatment. Some antiproliferative effects of iloprost-loaded platelets given i.v. during injury have also been observed. Whereas the incorporation of [3H]-thymidine into aorta intima-media DNA at 3 days post injury was 62-fold higher in balloon injured rats than in control sham operated rats, thymidine incorporation into intima/media of rats which had received iloprost loaded platelets during injury was reduced as compared with rats subjected only to the injury procedure. The reduction was only of near significance, however, but at 14 days after injury the total DNA content of the aorta intima/media of rats given iloprost loaded platelets during injury was significantly reduced. Although iloprost loaded platelets can clearly inhibit excessive platelet deposition, other encapsulated agents may have greater anti-proliferative effects. These studies have shown that drug loaded platelets can be targeted to injured arteries, where they may be retained as depots for local release. We believe this novel drug delivery protocol may have therapeutic potential in reducing the incidence of occlusion and restenosis after angioplasty and thrombolysis treatment. Electro-encapsulation of drugs into platelets is a simple procedure and, using autologous and fully biocompatible and biodegradable platelets as delivery vehicles, might overcome some of the immunological and toxicological problems which have been encountered with other delivery vectors such as liposomes, microbeads, synthetic microcapsules and antibodies.


2010 ◽  
Vol 13 (4) ◽  
pp. 91-98
Author(s):  
Tuan Dinh Phan ◽  
Binh Thien Nguyen ◽  
Dien Khanh Le ◽  
Phuong Hoang Pham

The paper presents an application the research results previously done by group on the influence of technological parameters to the deformation angle and finish surface quality in order to choose technology parameters for the incremental sheet forming (ISF) process to produce products for the purpose of rapid prototyping or single-batch production, including all steps from design and process 3D CAD model, calculate and select the technological parameters, setting up manufacturing and the stage of post-processing. The samples formed successfully showed high applicability of this technology to practical work, the complex products with the real size can be produced in industries: automotive, motorcycle, civil...


Author(s):  
A. N. Bozhko

Computer-aided design of assembly processes (Computer aided assembly planning, CAAP) of complex products is an important and urgent problem of state-of-the-art information technologies. Intensive research on CAAP has been underway since the 1980s. Meanwhile, specialized design systems were created to provide synthesis of assembly plans and product decompositions into assembly units. Such systems as ASPE, RAPID, XAP / 1, FLAPS, Archimedes, PRELEIDES, HAP, etc. can be given, as an example. These experimental developments did not get widespread use in industry, since they are based on the models of products with limited adequacy and require an expert’s active involvement in preparing initial information. The design tools for the state-of-the-art full-featured CAD/CAM systems (Siemens NX, Dassault CATIA and PTC Creo Elements / Pro), which are designed to provide CAAP, mainly take into account the geometric constraints that the design imposes on design solutions. These systems often synthesize technologically incorrect assembly sequences in which known technological heuristics are violated, for example orderliness in accuracy, consistency with the system of dimension chains, etc.An AssemBL software application package has been developed for a structured analysis of products and a synthesis of assembly plans and decompositions. The AssemBL uses a hyper-graph model of a product that correctly describes coherent and sequential assembly operations and processes. In terms of the hyper-graph model, an assembly operation is described as shrinkage of edge, an assembly plan is a sequence of shrinkages that converts a hyper-graph into the point, and a decomposition of product into assembly units is a hyper-graph partition into sub-graphs.The AssemBL solves the problem of minimizing the number of direct checks for geometric solvability when assembling complex products. This task is posed as a plus-sum two-person game of bicoloured brushing of an ordered set. In the paradigm of this model, the brushing operation is to check a certain structured fragment for solvability by collision detection methods. A rational brushing strategy minimizes the number of such checks.The package is integrated into the Siemens NX 10.0 computer-aided design system. This solution allowed us to combine specialized AssemBL tools with a developed toolkit of one of the most powerful and popular integrated CAD/CAM /CAE systems.


2019 ◽  
Author(s):  
Kristina Eriksen ◽  
Bjarne Nielsen ◽  
Michael Pittelkow

<p>We present a simple procedure to make an augmented reality app to visualize any 3D chemical model. The molecular structure may be based on data from crystallographic data or from computer modelling. This guide is made in such a way, that no programming skills are needed and the procedure uses free software and is a way to visualize 3D structures that are normally difficult to comprehend in the 2D space of paper. The process can be applied to make 3D representation of any 2D object, and we envisage the app to be useful when visualizing simple stereochemical problems, when presenting a complex 3D structure on a poster presentation or even in audio-visual presentations. The method works for all molecules including small molecules, supramolecular structures, MOFs and biomacromolecules.</p>


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