70960-98-4Relevant academic research and scientific papers
Fully automated radiosynthesis of [1-(2-[18F]fluoroethyl),1H[1, 2,3]triazole 4-ethylene] triphenylphosphonium bromide as a potential positron emission tomography tracer for imaging apoptosis
Haslop, Anna,Gee, Antony,Plisson, Christophe,Long, Nicholas
, p. 313 - 316 (2013)
A novel phosphonium salt bearing a fluorine-18 labelled triazole has been designed as a potential imaging agent for apoptosis. The radiosynthesis of [1-(2-[18F]fluoroethyl),1H[1,2,3]triazole 4-ethylene] triphenylphosphonium bromide ([18F]MitoPhos-01) has been carried out on a fully automated system in a two-step reaction. Radiolabelling an ethyl azide and then carrying out a copper-mediated 1,3-cycloaddition reaction has allowed for total synthesis time to be slightly more than 1 h from aqueous [18F]fluoride. After purification by HPLC, the average radiochemical yield was determined to be 9% (not decay corrected); the specific activity was on average 70 GBq/μmol at the end of synthesis, and the radiochemical purity was >99%. A novel phosphonium salt bearing a fluorine-18 labelled triazole has been designed as a potential imaging agent for apoptosis. The radiosynthesis of [1-(2-[18F]fluoroethyl),1H[1,2,3]triazole 4-ethylene] triphenylphosphonium bromide ([18F]MitoPhos-01) has been carried out on a fully automated system in a two-step reaction, with the average radiochemical yield determined to be 9% (not decay corrected); the specific activity being around 70 GBq/μmol at the end of synthesis and the radiochemical purity above 99%. Copyright
Annulation of thioimidates and vinyl carbodiimides to prepare 2-aminopyrimidines, competent nucleophiles for intramolecular alkyne hydroamination. Synthesis of (-)-crambidine
Perl, Nicholas R.,Ide, Nathan D.,Prajapati, Sudeep,Perfect, Hahdi H.,Duron, Sergio G.,Gin, David Y.
supporting information; experimental part, p. 1802 - 1803 (2010/04/24)
(Chemical Presented) A convergent synthesis of (-)-crambidine is reported. The sequence capitalizes on two novel key transformations, including a [4+2] annulation of thioimidates with vinyl carbodiimides and an alkyne hydroamination employing 2-aminopyrimidine nucleophiles. Copyright
Synthesis of aplyolide A, ichthyotoxic macrolide isolated from the skin of the marine mollusk Aplysia depilans
Spinella,Caruso,Martino,Sessa
, p. 1971 - 1973 (2007/10/03)
A convergent pathway is described for the synthesis of (S)-aplyolide A (1) using ethyl (S)-lactate as chiral source. Key steps of the synthesis are two couplings between copper(I) alkynides and propargylic halides for the formation of skipped diyne systems and were performed with an improved procedure based on the use of cesium carbonate as base for alkynide preparation.
Search for New Membrane-active Substances: Synthesis of Tropan-3-ols with Alkyl, Alkenyl and Alkenynyl Groups at the Bridgehead
Dharanipragada, Ramalinga,Fodor, Gabor
, p. 545 - 550 (2007/10/02)
The synthesis of tropan-3-ols with alkyl, alkenyl and alkynyl groups at the bridgehead is described.The new compounds have been considered as new membrane-active substances that would serve as model compounds for histrionicotoxin (1).Application of the Noyori route to 2-substituted pyrroles was unsuccessful.In order to avoid difficulties in obtaining individual long-chain 4-keto aldehydes for the Robinson condensation of each new model compound a key tropane intermediate (8) was prepared instead.The first attempts to extend the chains of the mesyl ester of the diol (8b) and iodomethyltropanol (9b) by Grignard type coupling failed.Therefore we embarked on a Wittig reaction of the tropane-1-carbaldehyde (11) synthesized in high yield from the diol (8).Indeed, both pent-1-enyl- and pentyl-tropanols, (12) and (13) were obtained.Coupling with an acetylenic phosphorane led to the pent-1-enynyltropanol (14).A further new key compound, namely 3β-acetoxytropan-1-ylacetaldehyde (15) was also synthesized as a precursor to conjugated tropanyl enynes which would more closely resemble the natural product (1).
