ChemInform Abstract: Synthesis and Antiparasitic Activities of Amidinic Azolated Derivatives.

Abstract

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Rapid Access to Chroman‐3‐ones through Gold‐Catalyzed Oxidation of Propargyl Aryl Ethers

“…Chroman‐3‐one is an important structural motif and its derivatives have served as key intermediates in the total synthesis of natural products such as miroestrol,1 (+)‐myristinin A,2 and afzelechin,3 as well as in accessing a range of bioactive chromans for managing various diseases including hypertension,4 HIV,3 sexual dysfunction,5 and melanoma 6. In their 1991 review,7 Danan and Kirkiacharian concluded that there was a lack of efficient synthetic methods for this structure. Since then, little progress8 has been made.…”

“…To date, the 20 year old statement still remains largely true. Invariably, these compounds are prepared through multistep routes7, 9 from basic chemicals. For example, a typical route starts from basic condensation of salicylaldehyde with acrylonitrile to form 2 H ‐chromene‐3‐carbonitrile under refluxing conditions with subsequent basic hydrolysis, acidification, formation of acyl azide, Curtius rearrangement, and acidic hydrolysis of the resulting vinyl isocyanate 1.…”

Bis[2-(1H-benzotriazol-1-yl)acetonitrile-κN3]dibromidocopper(II)

“…For the synthesis of the organic ligand, see: Danan et al (1997); Xu & Ye (2007). For the structure of a similar complex, see : Hang & Ye (2008).…”

“…The ligand, 2-(1H-benzo [d][1,2,3]triazol-1-yl)acetonitrile, was synthesized by the reaction of benzotriazole and bromoacetonitrile according to the procedure described in the literature [Danan et al (1997)]. …”

Benzimidazole derivatives endowed with potent antileishmanial activity

“…To meet the need of novel more efficacious, safe and unexpensive drugs to treat leishmaniasis, a number of studies are ongoing, exploring a wide chemical space from several classes of natural products 5 and or their semi-synthetic derivatives (sterols 5 , mono-, sequi-, di-and tri-terpens 6 , alkaloids 7 , flavonoids 8 , etc.) to the most diversified synthetic compounds, from the simple chloroacetoanilides 9 , to organometallics 10a (as auranofin 10b ), aryldiselenides 11 , adamantylidene alkyl phosphocoline 12 and a variety of heterocycles 13 , particularly indole 14 , indazole 15 , benzotriazole 16 and benzimidazole [17][18][19][20] derivatives. Examples of these compounds are depicted in Figures 2 and 3.…”