Aspects of yield and specific activity of (n,γ) produced 177Lu used in targeted radionuclide therapy

¹⁷⁷Lu-labeled receptor avid peptides and monoclonal antibodies have been effectively used in targeted tumor therapy, owing to the ideally suited decay properties and favourable production logistics of ¹⁷⁷Lu [T_½ = 6.65 days; E_β(max) = 497 keV (78.6 %); E_γ = 208 keV (11.0 %)]. The specific activity of ¹⁷⁷Lu produced by the (n,γ) route is one of the important criteria, which determines the efficacy of ¹⁷⁷Lu-labeled receptor-avid biomolecules. The present article highlights that the specific activity of (n,γ) produced ¹⁷⁷Lu cannot be calculated by simply dividing the produced activity by the mass of the target irradiated, unlike other (n,γ) produced medical radioisotopes and there is a significant enhancement of specific activity due to the burn up of the Lu target during irradiation, which is an added advantage towards the utilization of ¹⁷⁷Lu in receptor specific therapeutic radiopharmaceuticals.     

Synthesis of structurally diverse bis-peptide oligomers

We have developed second-generation monomers 1 and 2 and improved conditions for rapidly and simultaneously closing multiple diketopiperazines on solid support. These new conditions involve either the microwave heating of a suspension of solid-supported amino-tetrafluoropropyl esters in acetic acid/triethylamine catalyst solution or continuous flow of catalyst solution through the resin, heated in a flow cell apparatus. We demonstrate that the new monomers 1 and 2 can be combined with the new conditions easily to synthesize previously inaccessible hetero and homo spiro ladder oligomers 3 and 4 and others.     

Three Component Reaction: An Efficient Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones and Thiones Using Heterogeneous Catalyst

Fluoroboric acid supported on silica gel (HBF₄‐SiO₂) catalyzes efficiently the three component condensation of an aldehyde, a 1,3‐dicarbonyl compound and urea or thiourea to afford the corresponding 3,4‐dihydropyrimidin‐ 2(1H)‐ones and thiones in high yields. The ambient conditions, fast reaction rates, and excellent product yields are the important characteristics of this reaction.     

A facile method for the synthesis of substituted pyrazolo[3,4-c]pyridines

Methods for a facile high-yielding synthesis of substituted pyrazolo[3,4-c]pyridines from 2-bromo-5-fluoropyridine are described, along with a brief mechanistic discussion for the key cyclization step. The methods utilize inexpensive commercially available starting materials and unlike previous methods, are more suitable for SAR work and scale-up.     

Mixed metal MgO–ZrO2 nanoparticle‐catalyzed O‐tert‐Boc protection of alcohols and phenols under solvent‐free conditions

An environmentally benign method for O‐tert‐Boc protection of alcohols and phenols catalyzed by MgO–ZrO₂ nanoparticles under solvent‐free conditions is described. A variety of phenols, alcohols (aliphatic and aromatic) were converted to corresponding O‐tert‐Boc products in good to excellent yield (50–95%). The present protocol is expedient, simple, and efficient under solvent‐free conditions. The MgO–ZrO₂ Nps are easily prepared from inexpensive precursors, and are reusable, recyclable and chemoselective. Copyright © 2012 John Wiley & Sons, Ltd.     

Platinum (IV) thiohydrazide, thiodiamine and thiohydrazone complexes: a spectral, antibacterial and cytotoxic study

Some platinum (IV) complexes [Pt(L)2Cl2] [where, L=2-aminopyridine-N-thiohydrazide (L1), (2-aminopyridine-N-thio)-1,3-propanediamine (L2), benzaldehyde-2-aminopyridine-N-thiohydrazone (L3) and salicylaldehyde-2-aminopyrtidine-N-thiohydrazone (L4)] have been synthesized. The thiohydrazides, thiodiamine and thiohydrazones can exist as thione-thiol tautomer and coordinate as a bidentate N-S ligand. The ligands found to act in monobasic bidentate fashion. Analytical data reveals that metal to ligand stoichiometry is 1:2. The complexes have been characterized by elemental analysis, IR, mass, electronic and 1H NMR spectroscopic studies. In vitro antibacterial and cytotoxic study have also been carried out for some complexes.     

Intra-Specific Variation of Precocene I in the Wild Population of Ageratum conyzoides L. from the Western Himalayas

JPC – Journal of Planar Chromatography – Modern TLC -