Letters in Organic Chemistry - Volume 15, Issue 11, 2018

This work describes an efficient and new catalyst for the one-pot synthesis of organic disulfides/ sulfides via a palladium catalyst in the presence of PPh3 ligands for domino cross-coupling reaction of aryl halides and thiourea and then sulfur-transformation. Finally, the generated aryl thiolate converts to disulfide at normal oxidative and atmospheric conditions in DMF/water. However, thiols convert to unsymmetrical sulfides by Read More

In the paper, we wish to report an efficient one-pot synthesis of α-alkylated β-ketothioesters based on H2SO4-catalyzed tandem alkylation/hydrolysis reaction between acyclic α-oxo ketene dithioacetals and alcohols. It was shown that the tandem reaction could efficiently occur in the presence of 5 mol% H2SO4 at room temperature in CH3CN, affording the desired α-alkylated β-ketothioesters in excellent yields. Read More

Achiral N9-benzylguanine derivatives with alkene moieties attached to the benzyl group were synthesized with the intent of targeting a covalently linked unimolecular quadruplex using olefin cross-metathesis. Three N9-(3,5-bis(alkenyloxy)benzyl)-guanine derivatives were synthesized and shown to form stable G-quartet structures in the presence of a central cation. Upon the addition of K+, the guanine derivative, N9-(3,5-Bis(pent Read More

Multi component reactions (MCRs) are emerged as the most an effective and efficient tool in modern synthetic organic chemistry in the recent years. Syntheses of complex and diverse organic molecules from simple and readily available starting materials in a single step can be achieved by MCRs. We achieved PMA-SiO2 catalysed synthesis of 1,8-dioxodecahydroacridines through multi component reactions (MCRs) of 5, 5-di Read More

Inherently chiral pyrazine derivative of calix[4]arene was synthesised from calixquinone derivative and ethylenediamine in the presence of copper (II) acetate as a racemate. The obtained molecule was characterised by various spectroscopic methods such as: 1H NMR, 13C NMR, HH-COSY and IR spectroscopies.

Here, we report a simple and efficient method for the synthesis of different unsymmetrical N,N'-disubstituted urea and N-substituted urea derivatives using L-Proline as a green catalyst. The methodology is applicable for synthesizing various derivatives of phenylurea, diphenyl urea with excellent yield at mild condition.

A series of novel N-substituted-2-amino-3,4,5-trimethoxybenzoylindoles was synthesized and assessed against human cancer cell lines of breast (MCF-7) and colon (HT-29). The two derivatives 7a and 11a, in which the hydrogen atom at position 1 was substituted by a methyl and a benzoyl group respectively, showed significant cytotoxic activity GI50 against MCF-7 (0.045 μM), HT-29 (4.25 μM) and MCF-7 (0.035 μM) HT-29 (0. Read More

1,3,4-oxadiazole-2-thiole 6 was obtained from 4-(2-fluoro-4-nitrophenyl)morpholine (2) by the reduction of its nitro group and the sequential treatment of the resulting amine with ethyl bromoacetate, hydrazine hydrate, and carbon disulfide. The treatment of hydrazide 5 with isothiocyanates produced the corresponding carbothioamides 10a,b. The synthesis of triazoles 11a,b was achieved by intramolecular cy Read More

The catalytic asymmetric synthesis of terminal epoxides and 1,2-diols via a hydrolytic kinetic resolution of racemic terminal epoxides using a new bimetallic chiral salen CoIII complex incorporated with La(OTf)3 as a catalyst is reported. The new bimetallic chiral salen CoIII complex bearing La(OTf)3 was prepared in a one-pot procedure by activation and bimetallic complex formation from the inactive Jacobsen chiral salen C Read More

Four new pyran-based cembranoidal diterpenes (1-4) were isolated from the Red Sea softbodied coral Sarcophyton glaucum. Sarcoglauphine A (1) and B (2) are conformers with respect to the dihedral angle between H-7 and the pair of H-6a, 6b, while sarcotrocheliol-B acetate (3) and sarcotrochelione (4) are bicyclic cembranoids. The chemical structures of the isolated compounds were elucidated using spectroscopic Read More

In this study, the chemical constituents of the aerial parts of Archidendron bauchei (Jack) I. Niels have been investigated for the first time. Ten antioxidant compounds have been isolated and identified from the extracts, in which the amounts of methyl gallate and quercetin are fairly large with around 1.588 ± 0.014 and 3.145 ± 0.049 mg/g, respectively. In addition, the antioxidant potential of all extracted fractions and the i Read More

Prostate cancer is the most common malignancy in men. For the development of potential anti-prostate cancer agents, a series of arylpiperazine derivatives was synthesized based on previous studies. The target compounds were synthesized via three-step reaction and their in vitro cytotoxic efficacies against a panel of three human prostate cancer cell lines (PC-3, LNCaP, and DU145) and one normal prostate epithelial cell lin Read More