New novel derivatives of N-((5-((6-oxido-6-(4 substituted phenoxy)-4,8-dihydro-1H-[1,3,2] dioxaphosphepino [5,6-c]pyrazol-1-yl) methyl)-1,3,4-thiadiazol-2-yl)carbamoyl) substituted benzene sulfo namides (7a-o as depicted in scheme) were Synthesized by condensation reaction of 4substituted Phenyl phosphorodichloridates (6a-c) and N-((5-((4,5-bis(hydroxymethyl)-1H-pyrazol-1-yi)methyl)1,3,4-thiadi...

A detailed study was made of methyl sterols involved in cholesterol biosynthesis in adult brain following intracerebral injection of [ZJ4C]mevalonic acid and incubation of this cholesterol precursor with adult brain cell-free preparations. High specific activity lanosterol, 4,4-dimethyl-&-cholestaS(9)-24-dien-3P-01, 4a-methyl-5a-cholesta-‘7,24-dien-3/3-o1, and Sa-cholesta-7,24-dien-3/?-ol were ...

Methods have been described for the preparation of tritiated carcinogenic polycyclic aromatic hydrocarbons of high specific activity by the Wilzbach method. A large num ber of highly radioactive impurities were produced during the exposure to tritium gas, and extensive purification was required. This was achieved by column chromatography followed by various paper Chromatographie systems with so...

reaction of tryptamine 1 with dimethyl -3-methoxyallylidenemalonate 2 afforded n?-[4,4-bis (methoxycarbonyl)-1,3-butadienyl] tryptamine 3 which in combination with acetylchloride and pyridine in dichloromethane gave n?, n?-[acetyl]-[(4,4-dinethoxycarbonyl) 1,3butadienyl] tryptamine 4. treatment of 3 with sodium hydroxide afforded 2h[n-(3-indolyl) ethyl] 2-oxo-3-methoxycarbonyl-1-pyridine 5. cyc...

for the carcinogenic activity of the azo dyes re lated to 4-dimethylaminoazobenzene (DAB) has been well established (13, 15, 80, 31). Further more, the N-dimethyl and N-monomethyl dyes studied have essentially the same carcinogenic ac tivities, while the primary aminoazo dyes are much less active (5, 16) and apparently owe their carcinogenicity to a small amount of N-methyla tion in t@ivo(16). ...

Solid-phase microextraction (SPME) is directly integrated with low temperature plasma ionisation mass spectrometry to rapidly detect organophosphate chemical warfare agent simulants and their hydrolysis products in chemical mixtures, including urine. In this sampling and ionization method, the fibre serves: (i) to extract molecules from their native environment, and (ii) as the ionization elect...

Methylphosphonate synthase is a non-heme iron-dependent oxygenase that converts 2-hydroxyethylphosphonate (2-HEP) to methylphosphonate. On the basis of experiments with two enantiomers of a substrate analog, 2-hydroxypropylphosphonate, catalysis is proposed to commence with stereospecific abstraction of the pro-S hydrogen on C2 of the substrate. Experiments with isotopologues of 2-HEP indicate ...

Transition metal‐free Claisen‐type condensation between two different amides was developed. N ‐phenyl‐ ‐tosylbenzamide derivatives reacted with enolizable such as ‐methyl pyrrolidinone and , ‐dimethyl acetamide in the presence of NaHMDS to give their corresponding β ‐ketoamides moderate‐to‐good yields.

A furanoside phosphite-phosphoroamidite and diphosphoroamidite ligand library L1-L5a-f was tested in the asymmetric Rh-catalyzed hydrogenation of α,β-unsaturated carboxylic acid derivatives and enamides. Enantioselectivity depended strongly on the ligand parameters. High enantioselectivities were obtained in the reduction of dimethyl itaconate (up to >99% ee), α-dehydroamino acid esters (up to ...