Synthesis of Active Metabolites of Carvedilol,an Antihypertensive Drug

A simple synthetic route for active metabolites of carvedilol is reported. The metabolites 4′-hydroxycarvedilol and 5′-hydroxycarvedilol have exhibited high activity for β-blockade. We have disclosed syntheses of 4′-hydroxycarvedilol and 5′-hydroxycarvedilol from commercially available vanillin and isovanillin, respectively.     

High proton conductivity of water channels in a highly ordered nanowire

A proton-conductive material based on a crystalline assembly of trimesic acid and melamine (TMA?M, see picture) is reported. Because of the ordered structure of the assembly, the water-saturated proton conductivity for the TMA?M assembly is 5.5?S?cm(-1) , which is the highest proton conductivity measured to date. This exceptionally high conductivity and low-cost fabrication of the material make applications feasible for fuel-cell devices.     

Computer simulation of proton channelling in silicon

The channelling of 3 MeV protons in the 〈110〉 direction of silicon has been simulated using Vineyard model taking into account thermally vibrating nuclei and energy loss due to ion-electron interactions. A beam made up of constant energy particles but with spatial divergence has been simulated for the purpose. The values of the minimum scattering yield and half width of the channelling dip are shown to be depth sensitive and agree well with the measured values. The dependence of yield on the angle of incidence has been found to give information of all three types of channelling. The critical angles for the three types of channelling and wavelength of planar oscillations are consistent with the previous calculations.     

Energy dependence of multiplicity in proton-nucleus collisions and models of multiparticle production

This is a continuation of our earlier investigation (Gurtuet al 1974Phys. Lett. 50 B 391) on multiparticle production in proton-nucleus collisions based on an exposure of emulsion stack to 200 GeV/c beam at the NAL. It is found that the ratioR _em = 〈n _s〉/〈n _ch〉, where 〈n _ch〉 is the charged particle multiplicity in pp-collisions, increases slowly from about 1 at 10 GeV/c to 1·6 at 68 GeV/c and attains a constant value of 1·71 ± 0·04 in the region 200 to 8000 GeV/c. Furthermore,R _em = 1·71 implies an effectiveA-dependence ofR _A =A ^0.18,i.e., a very weak dependence. Predictions ofR _em on various models are discussed and compared with the emulsion data. Data seem to favour models of hadron-nucleon collisions in which production of particles takes place through adouble step mechanism,e.g., diffractive excitation, hydrodynamical and energy flux cascade as opposed to models which envisage instantaneous production.     

Novel compounds for the synthesis of cefdinir

Preparation of two new compounds 2‐mercapto‐5‐methyl‐1,3,4‐thiadiazolyl‐(Z)‐2‐(2‐amino‐4‐thiazolyl)‐2‐trityloxyiminoacetate ( 14 ) and 2‐mercapto‐5‐methyl‐1, 3,4‐thiadiazolyl‐ (Z)‐2‐(2‐amino‐4‐thiazolyl)‐2‐acetyloxyiminoacetate ( 12 ) and their use in the preparation of 7β‐[(Z)‐2‐(2‐amino‐4‐thiazolyl)‐2‐hydroxyiminoacetamido]‐3‐vinylcephem‐4‐carboxylic acid, also known by the generic name Cefdinir ( 1 ) has been accomplished in a single step by coupling with 7‐amino‐3‐vinylcephem‐4‐carboxylic acid ( 7 ) with purity of greater than 99% by HPLC.     

Discussion on a possible neutrino detector located in India

We have identified some important and worthwhile physics opportunities with a possible neutrino detector located in India. Particular emphasis is placed on the geographical advantage with a stress on the complimentary aspects with respect to other neutrino detectors already in operation.     

Novel azaandrostane derivatives for the synthesis of 17β‐(N‐tert‐butyl carbamoyl)‐4‐aza‐5α‐androst‐1‐ene‐3‐one

A new industrially viable process for the preparation of 1β‐(N‐tert‐butyl carbamoyl)‐4‐aza‐5α‐androst‐1‐ene‐3‐one, also known by the generic name finasteride ( 6 ) from the new azaandrostane derivatives such as 1β‐(N‐tert‐butyl carbamoyl)‐4‐benzoyl‐4‐aza‐5α‐androstane‐3‐one ( 4 ), 1β‐(N‐tert‐butyl carbamoyl)‐4‐benzoyl‐4‐aza‐5α‐androst‐1‐ene‐3‐one ( 5 ) is reported. In this process, benzoyl group is demonstrated as a novel protecting group for lactamic NH group. The structures of newly prepared compounds were established on the basis of spectral data (IR, ¹H‐NMR, and MS).     

Novel approach for the conversion of natural Δ3 cephalosporin derivatives into corresponding Δ2 cephalosporin derivatives

A simple one pot synthetic method for the isomerization of cephem double bond from the natural 3‐position to 2‐cephem positions is affected by silylation. Thus cephalosporin acids are treated with Ntrimethylsilylacetamide (MSA) or N,O‐bis(trimethylsilyl)acetamide (BSA) and the resulting silyl esters are treated with triethylamine at ambient temperature in the same pot to afford Δ²‐cephalosporins, which are potentially related compounds in cephalosporin antibacterial compounds.