3-N-([18F]fluoroalkyl)spiperone derivatives (2, 3) can be prepared by N-alkylation of spiperone (1) with fluoroalkyl halides. The fluoroalkylating species 2-[18F]fluoroethyl bromide (7), 3-[18F]fluoropropyl bromide (8) and 4-[18F]fluorobutyl bromide (9) were prepared by [18F]fluoride ion displac...

No-carrier-added (NCA)3-(2′-[18F]fluoroethyl)spiperone (5), a new dopamine receptor-binding radiopharmaceutical for positron emission tomography, was synthesized by two different methods. Alkylation of the amide nitrogen in spiperone by NCA [18F]fluorobromoethane in the presence of a strong bas...

The ligands currently used for PET studies of the dopamine receptor are fluorine-18-labeled spiperone (FSp) and carbon-11 or fluorine-18-labeled N-methyl-spiperone. All three of these ligands have drawbacks in either their chemical preparation or their biological behavior. We have previously pre...

The synthesis of 3-(2′-[18F]fluoroethyl)spiperone (1c), a radiotracer useful for imaging the brain dopamine receptor system in vivo using positron emission tomography, is described. Precursors of 1c, the functional 3-N-alkyl derivatives of spiperone (4), were prepared by the alkylation of the a...

3-N-(2-[18F]-fluoroethyl)-spiperone ([18F]-FESP) was synthesized at high specific activity by condensation with 2-[18F]-fluoroethyltosylate (35 TBq/mmol). In vivo binding studies in baboons by positron emission tomography exhibited regioselective uptake in the striatum which was saturable with t...

Increased circulating 11β-hydroxyprogesterone (11OHP4), biosynthesised in the human adrenal, is associated with 21-hydroxylase deficiency in congenital adrenal hyperplasia. 17α-hydroxyprogesterone levels are also increased, with the steroid’s metabolism to dihydrotestosterone in the backdoor ...

5(10)-Estrene-3β,17α-diol is an essential reference material for doping analysis in horse-racing laboratories. It is used to detect misuse, for doping purpose, of the pregnancy status in the mare. Its stereoselective synthesis from 17β-estradiol-3-methyl ether (prepared from estrone or 17β-e...

Adsorption of endocrine disrupting chemicals (EDCs) such as 17α-ethynyl estradiol and β-estradiol on sp2 hybridized graphene oxide (GO) sheets as an efficient adsorbent was carried out. The effect of different experimental parameters such as the concentration of adsorbent and adsorbate as well...

There are quite substantial number of impurities related to dexamethasone or mometasone which cannot be made from respective Active Pharmaceutical Ingredients but from common intermediate 21-acetoxy-17α-hydroxy-16α-methyl-pregna-1,4,9(11)-triene-3,20-dione (12). As such, a robust and economica...

Various corticosteroids are prepared by using 11α,17α-diOH-progesterone (11α,17α-diOH-PROG) as an important intermediate and raw material. Hence, strains that can improve the yields of 11α,17α-diOH-PROG should be screened. Cunninghamella elegans CICC40250 was singled out from five common 1...

Relatively high abundance of 17α (H)-diahopane has been detected in source rock extracts in the Yabulai Basin, a lacustrine basin in northwest China. Gas chromatography-mass spectrometry (GC-MS), X-ray diffraction (XRD) and Field emission environment scanning electron microscope imaging (FE-ESE...

Chitosan nanoparticles conjugated with 17α-methyltestosterone (CS + MT) were used for studying their effect on the testicular development of Clarias batrachus during different reproductive phases. The size of chitosan nanoparticles was 127.2 nm and the nano-conjugated 17α methyltestosterone (1...

11α-Hydroxyprogesterone (11αOHP4) and 11β-hydroxyprogesterone (11βOHP4) have been reported to be inhibitors of 11β-hydroxysteroid dehydrogenase (11βHSD) type 2, together with 11β-hydroxytestosterone and 11β-hydroxyandrostenedione, and their C11-keto derivatives being inhibitors of 11βHS...

New water-soluble decasubstituted pillar[5]arenes containing glycine and glycylglycine fragments were synthesized and characterized. The UV, DLS and TEM study showed that interaction of self-associates of the glycylglycine derivatives with Bismarck brown Y produced particles of about 59 nm in size.

The removal of the synthetic dye Bismarck Brown Y (BBY) has been investigated by electro-Fenton process, using a RVC cathode to electrogenerate in situ hydrogen peroxide and regenerate ferrous ions as catalyst. The optimization of the process has been performed using Doehlert designs and the BBY...

Since overactivation of NMDA receptors is associated with neurodegenerative disorders, the design and development of subunit-selective NMDA receptor antagonists are of great interest. In order to avoid the formation of quinone-like intermediates as starting point for degradation the benzylic OH ...

A reaction of (S)-2-benzyl-2-(α-methylbenzyl)amino-1,3-propanediol (S)-4a and 2-chloroethyl chloroformate, and the subsequent addition of DBU gave (4R,αS)-4-benzyl-4-hydroxymethyl-3-(α-methylbenzyl)-2-oxazolidinone (4R)-5a (92% de) via a diastereoselective asymmetric desymmetrization process....

Hydroxymethyl ketones are useful auxiliaries in organic synthesis and are also found in several medicinal agents. N-Heterocyclic carbenes (NHCs) have been used in the literature in order to introduce the hydroxymethyl group into aromatic aldehydes in good yields, but they are not that successful...

The action of H-Phe-Ile-Tyr-His-Ser-Tyr-Lys-OH on the passive and active avoidance behavior and open-field activity of rats was studied after peripheral and intracerebroventricular administration. When applied before the test session, intracerebroventricular administration increased the avoidanc...

New tetraphenylsilane-containing polyarylate with two pendant benzyl ester groups was synthesized successfully by direct polycondensation from a new silicon-containing aromatic diacid monomer bis[p-(benzyloxycarbonyl)phenyl]-bis(p-carboxyphenyl)silane (BBCS) with p-dihydroxybenzene in pyridine, ...