1,721,182 research outputs found
Five-member-ring heterocycles by reacting enolates with dipoles
No full textThe synthetic utility of enolates in the heterocycles synthesis constitutes the main topic of this review. Appropriate enolates, in
a number of synthetic approaches, are easily formed in situ from a variety of carbonyl compounds (aldehydes, ketones, amides, etc.) and
used for the ring construction of (poly)substituted heterocycles. Often, the synthesis of five-membered rings such as isoxazoles, triazoles,
pyrazoles, etc. has been performed by using these intermediates through a two-step or even by one pot procedures. The selectivity and the versatility of enolates intermediates will be discussed, with particular attention to those methodologies useful for preparation of heterocycle
containing pharmacologically active molecule
Cyclooxygenase catalytic binding site demand for diarylisoxazole highly selective inhibition
No full textA new synthesis of b-phenylamino thioesters and beta-lactams via base-induced ring-opening of 2-phenyl-3-aryl-5-phenylthioisoxazolidines
No full text
Synthesis of 3-aryl-4,5-dihydro-5-hydroxy-1,2-oxazoles by reaction of substituted benzonitrile oxides with the enolate ion of acetaldehyde
No full textSelective reduction of aldehydes to the corresponding primary alcohols by lithium enolate of acetaldehyde
No full textCinnamaldehydes Via Hydroxyisoxazolidines: an Efficient Indirect Crossed Aldol Condensation
No full textNovel beta3 adrenergic receptor ligands: a patent review
No full textINTRODUCTION: Stimulation of the β(3)-adrenoceptor (β(3)-AR) is thought to be a valuable approach for the treatment of obesity, type 2 diabetes, heart failure, frequent urination, preterm labor, anxiety and depression. Therefore, the β(3)-AR is recognized as an attractive target for drug discovery. Simultaneous activation of the β(1)- and β(2)-AR can cause undesirable side effects such as increased heart rate and muscle tremors. Consequently, much effort has been directed towards the design and development of selective β(3)-AR agonists through original synthetic chemistry, extensive in vitro tests and detailed preclinical investigations to various phases of clinical trials. AREAS COVERED: SciFinder Scholar, PubMed, ISI web of Knowledge(SM), Espacenet, ClinicalTrials and Google have been used as the main sources for retrieving literature and patents filed since the discovery of β(3)-AR through to June 2010. This review discusses the enormous efforts made by private and public research laboratories to uncover β(3)-AR ligands and to prove their usefulness as drugs. EXPERT OPINION: Remarkable knowledge has been gained about the physio-pathological role of the β(3)-AR to date. Many highly potent and selective β(3)-AR ligands (agonists, antagonists and inverse agonists) have been discovered; however, further investigations are still needed to identify novel compounds acting as β(3)-AR ligands in order to adequately treat the diseases in which β(3)-AR is involved
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