A simple, practical, and regioselective synthetic protocol for the formation of pyrazoles was developed. Unlike all other previously reported reactions of nitroallylic acetates, this process was initiated by a SN2 reaction at the electrophilic γ site. A plausible mechanism for the cascade SN2-M...
The reaction of enol acetates with alcohols in the presence of a catalytic amount of a rhenium complex, such as ReBr(CO)5, produced the corresponding ketones and aldehydes in moderate to good yields. It was suggested that the preparation of an ether, an intermolecular dehydrated product, was the...
A novel direct alkylation of thiophenes via bis-coupling with vinyl acetates has been developed. To the best of our knowledge, this represents the first report of the iron-catalysed coupling of two thiophenes with vinyl groups. Utilizing earth-abundant, inexpensive, and non-toxic iron catalysts,...
In this paper, the title compound was synthesized from N-benzoyl-N′,N′-dibenzylthiourea ligand and potassium tetrachloroplatinate(II), and its interaction with human (HSA) and bovine (BSA) serum albumin was evaluated. Also, the crystal structure was determined from single-crystal X‐ray diffra...
1.1. Based on the scalp-recorded and computer-analyzed electroencephalogram, in high dosages antidepressant and in low dosages “psychostimulant” properties of mesterolone, a synthetic male hormone, were predicted.2.2. Open, uncontrolled clinical trials suggest dose-related antidepressant prope...
The possible effect of Mesterolone (Schering N.V., Brussels, Belgium) (lα-methyl-5-α-androstane-17β-ol-3-one) on semen quality and fertility of men with idiopathic oligoasthenospermia and/or teratozoospermia has been evaluated in a double-blind trial. The study included 52 patients who were t...
Two hundred fifty subfertile men with idiopathic oligospermia (count less than 20 million/ml) were treated with mesterolone (100–150 mg/day) for 12 months. Seminal analysis were assayed 3 times and serum follicle stimulating hormone (FSH) luteinizing hormone (LH) and plasma testosterone were as...
Mesterolone is an orally active synthetic androgen and has the general properties of androgens.
Fermentation of mesterolone (1) with Cunninghamella blakesleeana yielded four new metabolites, 1α-methyl-1β,11β,17β-trihydroxy-5α-androstan-3-one (2), 1α-methyl-7α,11β,17β-trihydroxy-5α-androstan-3-one (3), 1α-methyl-1β,6α,17β-trihydroxy-5α-androstan-3-one (4) and 1α-methyl-1β,1...
Mesterolone (1α-methyl-5α-androstan-17β-ol-3-one) is a synthetic anabolic androgenic steroid (AAS) with reported abuses in human sports. As for other AAS, mesterolone is also a potential doping agent in equine sports. Metabolic studies on mesterolone have been reported for humans, whereas lit...
Three new metabolites were obtained on incubation of androgenic steroid mesterolone (1) with Cunninghamella blakesleeana. These metabolites were identified as 1α-methyl-11β,14α,17β-trihydroxy-5α-androstan-3-one (2), 1α-methyl-7β,17β-dihydroxy-5α-androstan-3-one (3), and 1α-methyl,17β-...
Fluorescent derivatives of benzo[b]thiophene were synthesized by CC and CN palladium catalysed cross-couplings of bromobenzenes with 3-(benzo[b]thienyl)boronic acid and bromo- or aminobenzenes with 7-amino or 7-bromobenzo[b]thiophene, respectively. The photophysical behaviour of the coupled comp...
This study reports the identification of a chemical artifact occurring in the liquid chromatographic analysis of 3-butyn-2-one by means of the 2,4-dinitrophenylhydrazine (DNPH) method. Besides the expected derivatization reaction to the corresponding butynone DNPhydrazone, a rearrangement was ob...
The reactions of arylaldehydes with 3-butyn-2-one, methyl propiolate or propynenitrile in the presence of Lewis acids such as titanium(IV) bromide (TiBr4) or boron(III) tribromide (BBr3) (1.4 equiv.) can be drastically affected by the reaction temperature. When the reaction of arylaldehydes with...
The reaction of arylacetylenes 1 and N,N-dimethylformamide dimethylacetal (2a, DMF-DMA) afforded the corresponding arylpropargyl aldehydes 3 in moderate yields. Similarly, the reaction of 1 and N,N-dimethylacetamide dimethylacetal (2b, DMA-DMA) gave 4-aryl-3-butyn-2-ones 4.
In this paper, we show the substrate 4-(trimethylsilyl)-3-butyn-2-one is unstable, and can be easily cleaved into a carbonyl alkyne and trimethylhydroxysilane in aqueous buffer with pH above 6.0. However, this problem could be effectively solved by lowering the buffer pH. Meanwhile, the efficien...
The biocatalytic reduction of 4-(trimethylsilyl)-3-butyn-2-one to enantiopure (R)-4-(trimethylsilyl)-3-butyn-2-ol was successfully conducted with high enantioselectivity using immobilized whole cells of a novel strain Acetobacter sp. CCTCC M209061, newly isolated from kefir. Compared with other ...
The [3 + 2] cycloaddition of two acetylacetylenes with ruthenium azido complex [Ru]−N3 (1, [Ru] = (η5-C5H5)(dppe)Ru, dppe = Ph2PCH2CH2PPh2) is reported. The metal-bound heterocyclic complexes produced are triazolato complexes [Ru]N3C2H(COCH3) (2) and [Ru]N3C2(Ph)(COCH3) (3) from 3-butyn-2-one a...
An efficient method for the synthesis of 1-monosubstituted-1, 2, 3-triazoles from 2-methyl-3-butyn-2-ol under copper catalyst conditions has been developed through a one-step one-pot sequence. This method provides a concise and efficient pathway to synthesize 1-monosubstituted-1, 2, 3-triazole d...
A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was e...
About|Contact|Cas|Product Name|Molecular|Country|Encyclopedia
Message|New Cas|MSDS|Service|Advertisement|CAS DataBase|Article Data|Manufacturers | Chemical Catalog
©2008 LookChem.com,License: ICP
NO.:Zhejiang16009103
complaints:service@lookchem.com Desktop View