“…Chloromethylenedimethylammonium chloride (Vilsmeier reagent) 2 has been mostly used as an acid activator for the synthesis of esters [10], amides [11], β-sultams [12], diacylhydrazines [13], 1,3,4oxadiazoles [14], and β-lactams [15].…”
The first synthesis of 3‐phenothiazine‐β‐lactams is herein reported. Thirteen new derivatives of β‐lactams were synthesized using various Schiff bases and (phenothiazin‐10‐yl)acetic acid, which in turn was prepared starting from phenothiazine. The sole product of the Staudinger ketene–imine [2 + 2] cycloaddition reaction is the trans‐β‐lactam. All the synthesized compounds were characterized by elemental analyses and spectral (IR, 1H‐NMR, and 13C‐NMR) data.
“…Chloromethylenedimethylammonium chloride (Vilsmeier reagent) 2 has been mostly used as an acid activator for the synthesis of esters [10], amides [11], β-sultams [12], diacylhydrazines [13], 1,3,4oxadiazoles [14], and β-lactams [15].…”
The first synthesis of 3‐phenothiazine‐β‐lactams is herein reported. Thirteen new derivatives of β‐lactams were synthesized using various Schiff bases and (phenothiazin‐10‐yl)acetic acid, which in turn was prepared starting from phenothiazine. The sole product of the Staudinger ketene–imine [2 + 2] cycloaddition reaction is the trans‐β‐lactam. All the synthesized compounds were characterized by elemental analyses and spectral (IR, 1H‐NMR, and 13C‐NMR) data.
“…In the present work utilizing 4 as a synthon for cyclopentanoids, our first goal was to make a synthetically useful intermediate. Since our primary aim was piperidines, tosylation or mesylation of the diol 13 (see Scheme ) and subsequent treatment with an appropriate amine seemed the most straightforward method for achieving this. 1 Preparation of a Precursor ( 13 ) of Piperidines …”
Synthesis of five novel piperidine monoterpene alkaloids
(17−21) using the iridoid
glucoside
antirrhinoside (4) as a synthon is described. Two
strategies for their preparation were
investigated: the first possible pathway involved an intermediate
diol, 13, from which the
piperidine ring was expected to be constructed via reaction of its
ditosylate with an amine; the
second strategy involved a double reductive amination as the key step
to the piperidine ring,
which proved successful. The stereochemistry of C-5 and C-9 in the
obtained piperidine
monoterpenes was the same as that reported for α-skytanthine
(3), a known isolate from
Skytanthus
acutus (Apocynaceae).
“…Synthetic and methodology chemistry papers are generally much easier to write when compared to medicinal chemistry articles since there are typically fewer factors involved and the studies may be more succinct in scope. They cover a range of topics including correcting errors in the literature, , interesting rearrangements, − developing new reactions and devising new methodology, − detailed mechanistic studies, proof of stereochemistry, , and the characterization of natural products (although these are currently out of favor as sources of new leads for therapeutics) . Exploring the utility of new methodology devised in a project and its exemplification with nonconfidential substrates allows much earlier publication of the science, but these experiments have to be fitted in around project work. ,,, This can be achieved by working a little longer at the bench and by asking colleagues to help, with the promise that they will be considered for authorship in any forthcoming publication.…”
Section: Guidelines On Composing and Submitting Scientific
Articlesmentioning
Writing scientific articles is immensely rewarding but challenging. This Perspective provides the medicinal chemist with background and advice on the art and process of writing manuscripts and complements the instructions to authors provided by journals. Included are many tips that we wish we had known when we first started writing. Bibliometric data from seven medicinal chemistry journals between 2000 and 2019 are collated including Bioorganic and Medicinal Chemistry Letters and the Journal of Medicinal Chemistry. Although the overall number of articles has doubled, the output from 23 large pharma companies in the past decade has dropped significantly. Commentary is given on the entire process of writing original scientific articles, opinion articles, and reviews. Examples from our own papers and experience are shared including what typically motivates the writer, challenges commonly encountered, and how we find time to write. Finally, the benefits derived from much wider publishing of industrial medicinal chemistry are described.
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