Raymond I. Mori
Bio: Raymond I. Mori is an academic researcher. The author has contributed to research in topic(s): Thiadiazoles. The author has an hindex of 1, co-authored 1 publication(s) receiving 187 citation(s).
16 Feb 2001-Angewandte Chemie
TL;DR: It has been demonstrated that complex natural products like the alkaloids +/-)-oxomaritidine and (+/-)-epimaritidine can be prepared by a sequence of five and six consecutive polymer-assisted steps, respectively, and the potent analgesic compound (+/--epibatidine in twelve linear steps ten of which are based on functionalized polymers.
Abstract: As part of the dramatic changes associated with the need for preparing compound libraries in pharmaceutical and agrochemical research laboratories, industry searches for new technologies that allow for the automation of synthetic processes. Since the pioneering work by Merrifield polymeric supports have been identified to play a key role in this field however, polymer-assisted solution-phase synthesis which utilizes immobilized reagents and catalysts has only recently begun to flourish. Polymer-assisted solution-phase synthesis has various advantages over conventional solution-phase chemistry, such as the ease of separation of the supported species from a reaction mixture by filtration and washing, the opportunity to use an excess of the reagent to force the reaction to completion without causing workup problems, and the adaptability to continuous-flow processes. Various strategies for employing functionalized polymers stoichiometrically have been developed. Apart from reagents that are covalently or ionically attached to the polymeric backbone and which are released into solution in the presence of a suitable substrate, scavenger reagents play an increasingly important role in purifying reaction mixtures. Employing functionalized polymers in solution-phase synthesis has been shown to be extremely useful in automated parallel synthesis and multistep sequences. So far, compound libraries containing as many as 88 members have been generated by using several polymer-bound reagents one after another. Furthermore, it has been demonstrated that complex natural products like the alkaloids (+/-)-oxomaritidine and (+/-)-epimaritidine can be prepared by a sequence of five and six consecutive polymer-assisted steps, respectively, and the potent analgesic compound (+/-)-epibatidine in twelve linear steps ten of which are based on functionalized polymers. These developments reveal the great future prospects of polymer-assisted solution-phase synthesis.
01 Aug 1997-Pesticide Science
TL;DR: In this paper, a new class of chemicals called S-Methyl benzo[1,2,3]thiadiazole-7-carboxylic acid derivatives have been identified as a plant's own defence mechanisms.
Abstract: Systemic Acquired Resistance (SAR) is an inducible resistance mechanism in plants that, together with other defence mechanisms, provides broad-spectrum and long-lasting disease control. With novel screening techniques the benzo[1,2,3]thiadiazole-7-carboxylic acid derivatives have been identified as a new class of chemicals which stimulate the plant's own defence mechanisms. The synthesis and biological activities of various benzo[1,2,3]thiadiazoles and related structures are described. S-Methyl benzo[1,2,3]thiadiazole-7-carbothioate is the first synthetic chemical 'plant activator' that has been developed for this novel disease control concept.
01 Jan 2013-ChemMedChem
TL;DR: This Minireview, thiadiazoles are summarized according to their therapeutic potential, highlighting the versatility of this scaffold in medicinal chemistry and giving a brief introduction to their synthesis and diverse biological activities.
Abstract: Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities. In this Minireview, thiadiazoles are summarized according to their therapeutic potential, highlighting the versatility of this scaffold in medicinal chemistry. The unique properties of thiadiazoles are also discussed in relation to their potential effect on activity. Thiadiazole is a bioisostere of pyrimidine and oxadiazole, and given the prevalence of pyrimidine in nature it is unsurprising that thiadiazoles exhibit significant therapeutic potential. The sulfur atom of the thiadiazole imparts improved liposolubility, and the mesoionic nature of thiadiazoles makes these compounds better able to cross cellular membranes. By summarizing the thiadiazole-containing compounds reported in recent decades, we aim to give a brief introduction to their synthesis and diverse biological activities, such as anti-inflammatory, anticancer, antibacterial, antifungal, antiviral, antiparasitic, anticonvulsant, anticoagulant, antidiabetic, and to show the significant utility of the thiadiazole scaffolds in medicinal chemistry.
01 Jan 1972-Tetrahedron
TL;DR: In this paper, ausfuhrliche spektroskopische Charakterisierung der 1,2,3-Selenadiazole und 1,4-Diselenine wird gegeben.
Abstract: Zusammenfassung Aus Cycloalkanon-semicarbazonen bilden sich mit SeO 2 Cycloalkeno-1,2,3-selenadiazole. Ihre Thennolyse fuhrt zu Bis-cycloalkeno-1,4-diseleninen und Cycloalkinen, die mit Tetracyclon abgefangen werden konnen. Eine ausfuhrliche spektroskopische Charakterisierung der 1,2,3-Selenadiazole und der 1,4-Diselenine wird gegeben.
TL;DR: Aromatisch substituierte 1.3-Thiodiazole liefern bei Belichtung N2 and 1.4-Dithia-fulvene (z.B. VI).
Abstract: Aromatisch substituierte 1.2.3-Thiodiazole liefern bei Belichtung N2 und 1.4-Dithia-fulvene (z.B. VI). Die Struktur wurde durch Entschwefelung mit Raney-Nickel, Oxydation zu Disulfonen und deren Alkalispaltung sowie durch Reduktion bewiesen. Die 1.4-Dithia-fulvene bilden mit starken Sauren farblose Salze, die ein tropyliumanaloges Kation besitzen. Soweit sie unsubstituierten Wasserstoff enthalten, konnen sie zu tieffarbigen Salzen oxydiert werden. Di-substituierte 1.2.3-Thiodiazole geben neben 1.4-Dithia-fulvenen als weitere Belichtungsprodukte 1.4-Dithia-cyclohexadiene oder Thiophene, deren Konstitution und Eigenschaften beschrieben werden.