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Tetrahedron Letters | Year: 2010

A facile synthesis of 2,6-disubstituted pyrimidin-4-ones and 2,5,6-trisubstituted pyrimidin-4-ones from commercially available materials with application of microwave technology in key steps is described. © 2009 Elsevier Ltd. All rights reserved.

Tymoshenko D.O.,AMRI
Arkivoc | Year: 2011

In the past decade ring expansion of aziridines and aziridiniums fused to other rings has developed into an attractive alternative method to classical pyrrolidine, piperidine and azepine ring construction approaches. This short review provides an update on recent reports and demonstrates the usefulness and the efficiency of this approach. © ARKAT-USA, Inc.

Cioffi C.L.,AMRI
Bioorganic and Medicinal Chemistry Letters | Year: 2013

Schizophrenia is a devastating mental illness that afflicts nearly 1% of the world's population. Currently available antipsychotics treat positive symptoms, but are largely ineffective at addressing negative symptoms and cognitive dysfunction. Thus, improved pharmacotherapies that treat all aspects of the disease remain a critical unmet need. There is mounting evidence that links NMDA receptor hypofunction and the expression of schizophrenia, and numerous drug discovery programs have developed agents that directly or indirectly potentiate NMDA receptor-mediated neurotransmission. Several compounds have emerged that show promise for treating all symptom sub-domains in both preclinical models and clinical studies, and we will review recent developments in many of these areas. © 2013 Elsevier Ltd. All rights reserved.

Zych A.J.,AMRI | Wang H.-J.,AMRI | Sakwa S.A.,AMRI
Tetrahedron Letters | Year: 2010

A novel synthesis of 6-methyl-4-phenyl-5-substituted-3,4-dihydropyrimidin- 2(1H)-ones from 6-methyl-4-phenyl-5-halo-3,4-dihydropyrimidin-2(1H)-ones via the Suzuki-Miyaura reaction is reported. These previously unknown heterocyclic halides are easily prepared using the Biginelli multicomponent reaction followed by halodecarboxylation. The effect of varied substitution at the C-4 position on the cross-coupling reaction is also examined. © 2010 Elsevier Ltd. All rights reserved.

Song R.,AMRI | Lin W.,AMRI | Jiang Q.,AMRI
Tetrahedron Letters | Year: 2011

A convenient synthesis of 5-fluorofuran-2-carboxylic acid has been achieved in two steps and 56% total yield. Fluorodenitration of commercially available benzyl 5-nitrofuran-2-carboxylate utilizing potassium fluoride and catalytic tetraphenylphosphonium bromide in sulfolane at 140 °C for 2 h furnished benzyl 5-fluorofuran-2-carboxylate. Hydrogenolysis of benzyl 5-fluorofuran-2-carboxylate gave the title compound. © 2011 Elsevier Ltd. All rights reserved.

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