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| http://dx.doi.org/10.1080/00304948.2012.676823 | DOI Listing |
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Microwave-Assisted Selective Nucleopalladation-Triggered Cascade Process: Synthesis of Highly Functionalized 3-Chloro-1-indenes.
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Department of Chemistry and Chemical Sciences, Central University of Jammu, Rahya-Suchani (Bagla), District-Samba, J&K, Jammu 181143, India.
A nucleopalladation-triggered cascade transformation of internal alkynes bearing an amino nucleophile and an electrophilic enone was investigated under unconventional microwave-assisted conditions. Among the three possible pathways, the chloropalladation-triggered domino process proceeded selectively to furnish 3-chloro-1-indenes in good to excellent yields. The reactions under microwave irradiation were completed in 30 min, and the conventional heating required 3-5 h for completion.
View Article and Find Full Text PDFConcise Total Synthesis of (-)-Codeine.
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Department of Chemical Sciences, Indian Institute of Science Education and Research Kolkata, Mohanpur Campus, Kalyani, Nadia 741 246, West Bengal, India.
Codeine and morphine are among the few natural products that are used directly as drugs for medical treatment. However, the availability of these is widely dependent on natural resources. Herein, we report an efficient enantioselective seven-step synthesis of (-)-codeine starting from simpler starting materials.
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SCSOP, Via Bornò 5, 23896 Sirtori, Italy.
Cinacalcet (), sold as hydrochloride salt, is a calcimimetic drug which has been approved for the treatment of secondary hyperparathyroidism in patients with chronic renal disease and for the treatment of hypercalcemia in patients with parathyroid carcinoma. Here, an improved method for the synthesis of 3-(3-trifluoromethylphenyl)propanal (), a key intermediate for the preparation of , is described. The protocol required a Mizoroki-Heck cross-coupling reaction between 1-bromo-3-(trifluoromethyl)benzene and acroleine diethyl acetal, catalyzed by Pd(OAc) in the presence of nBuNOAc (tetrabutylammonium acetate), followed by the hydrogenation reaction of the crude mixture of products in a cascade process.
View Article and Find Full Text PDFFunctionalization of the imidazo[1,2-]pyridine ring in α-phosphonoacrylates and α-phosphonopropionates via microwave-assisted Mizoroki-Heck reaction.
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Institute of Organic Chemistry, Faculty of Chemistry, Lodz University of Technology, 116 Zeromskiego St, 90-924 Lodz, Poland.
A series of new phosphonocarboxylates containing an imidazo[1,2-]pyridine ring has been synthesized via the microwave-assisted Mizoroki-Heck reaction. The efficient modification of the imidazo[1,2-]pyridine ring has been achieved as late-stage functionalization, enabling and accelerating the generation of a library of compounds from a common precursor.
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Institute of Biological, Environmental and Rural Sciences (IBERS) , Aberystwyth University, Penglais Campus, Aberystwyth SY23 3DA , United Kingdom.
Sclareol, a plant-derived diterpenoid widely used as a fragrance and flavoring substance, is well-known for its promising antimicrobial and anticancer properties. However, its activity on helminth parasites has not been previously reported. Here, we show that sclareol is active against larval (IC ≈ 13 μM), juvenile (IC = 5.
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