Baccharis reticularia DC. is a plant species from the Asteraceae family that endemic to Brazil. Despite great importance of genus, no study has been carried out regarding either phytochemical composition B. or evaluation its larvicidal potential. Considering intrinsic immiscibility essential oils, this shows nanoemulsions containing phytochemically characterized oil and main constituent against Aedes aegypti. The major compound found was d-limonene (25.7%). inhibited acetylcholinesterase,...

A new catalytic route with potential practical interest to sustainable production of bio-additives from glycerol is described. Ethyl acetate was transesterified glycerol, in the ratio glycerol:EtOAc 1:10, at 25 or 90 ºC using 0.1 equiv. H2SO4 TsOH, as homogeneous catalysts. led total consumption 2 h. In equilibrium, attained 9 h, 100% yield a diacetin:triacetin (55:45) mixture formed. Using AmberlystTM 15 dry and 16 wet 1:30 reflux achieved 10h, respectively. The lower reactivity...

Despite the availability of alternative methods for drying tetrahydrofuran (THF), use still apparatus, wherein a THF solution containing Na-bezophenone ketyl is heated to reflux, remains widespread. We herein propose set procedures solve problems usually faced in applying this technique. Moreover, discussion made on chemical knowledge underlying such procedures. Safety and economy issues concerned with operation apparatus are also discussed.

Chiral nonracemic aminated nitroso acetals were synthesized via diastereoselective multicomponent [4 + 2]/[3 2] cycloadditions employing new ( S , E )-γ-nitrogenated nitroalkenes 5a–c as heterodienes, ethyl vinyl ether (EVE) a dienophile, and selected electron-deficient alkenes 1,3-dipolarophiles. The employment of different organic solutions LiClO 4 or LiCl promoter systems provided the respective with yields from 34–72% good levels diastereoselectivity. In addition, acetal 9c was...

The compound (±)-trans-4-hydroxy-6-propyl-1-oxocyclohexan-2-one [(±)-δ-lactone] was isolated from the plant Vitex cymosa Bertero, and determined to be active principle. present study aimed evaluate antinociceptive effect of (±)-δ-lactone elucidate its mechanism action. Mice were subjected in-vivo models acute pain (acetic acid-induced abdominal writhing, formalin hot-plate tests) open-field test. (±)-δ-Lactone, administered orally (6-900 µmol/kg), exerted a dose-dependent in acetic tests....

A concise and versatile formal synthesis to (+)-nephrosteranic acid was accomplished from a common nitroderivative 2 in sequence of six steps. The adduct obtained via highly syn-diastereoselective conjugate addition 1-dodecyl nitronate ion chiral enoate Z-5 (yield = 80%; de 95%), derived d-(+)-mannitol.

New chiral ( S,E )-γ- N , -dibenzylated nitroalkenes 2a–c were synthesized from natural L-(α)-amino acids in five steps with overall yields of 68–88%. The conjugate addition hydride, methoxide, nitronate and azide nucleophiles to led the corresponding 1,3-nitroamines 74–90% yield. cyanide anion 2a b was followed by HNO 2 elimination affording aminated acrylonitriles (73–98%). On other hand, reacted acetonitrile, via a [3 + 2]-cycloaddition which lost, providing 1,2,3-triazole derivative....

Pain is a major cause of distress, both physical and psychological. There continuous search for new pharmacologically active analgesic agents with minor adverse effects. Recently, the synthesis (-)-(2S,6S)-(6-ethyl-tetrahydropyran-2-yl)-formic acid [tetrahydropyran derivative (TD)] was described. The objective this study to investigate antinociceptive effects TD. Its activity compared morphine. TD morphine were evaluated in models inflammatory noninflammatory pain. (6-1200 μmol/kg,...

The synthesis to 3-nitropropionic acid 1 was easily accomplished, in two steps, from commercially available acrolein 60% yield. ethyl and methyl esters of were also obtained.

Abstract In this work we report the purification of a crude acetin mixture into mono‐, di‐ and triacetin by countercurrent chromatography. The process was initially tested on small, semi‐preparative scale (0.5 g) to determine its efficiency. then scaled up accommodate 2.5 g reaction products containing acetins. solvent system ethyl acetate/ n ‐butanol/water 1:0.2:1 used in all separation procedures. Mono‐, triacetins were separated similarly preparative runs.

New eco-friendly conditions for Finkelstein reaction employing homogeneous media or alumina-supported reagents, both solventless, were utilized in the bromohydrins and iodohydrins synthesis from 1,3-dichlorohydrin (1,3-DCH), obtained glycerol. Thus, trans-halogenation of glycerol-1,3-dichlorohydrin (1) media, using NaI, NaBr salts organic additives (TBAI, TBAB), led to four different glycerol halohydrins (2a, 2b, 3a, 3b) regular excellent conversions (43–96%) good selectivities 3a 2b....

The reactivity and diastereoselectivity of conjugate addition different nitronates ions to (R)-carvone was systematically studied. Michael adducts 2a-e were obtained in good yield 3,2-cis-3,5-trans selectivity. nitroadducts 2b,c transformed via Nef reaction into ketone derivatives 9,10 2b,d led alkylated 11,12, a denitration reaction.

New efficient and reproductive routes to production of 1,3-dihydroxyacetone (1), 1,3-dichloroacetone (6), 1,3-dibromoacetone (7) 1,3-diiodoacetone (8) from glycerol 1,3-dichlorohydrin (3) were developed.The synthesis 1 was processed in three steps 2 (1,3-selective chlorination 3, oxidation 3 6 subsequent di-hydroxylation) 51% overall yield.On the other hand, 7 8 produced via a trans-bromination trans-iodination, respectively, followed by hydroxylation steps, 38-52% yield.It used homogeneous...

Two innovative and efficient routes were developed to produce glycerol-alkyl ethers employing Williamson reaction conditions in a heterogeneous medium. Thus, the ion exchange resin Amberlyst A26TM −OH form KOH supported on alumina (KOH/Al2O3) used as basic solid reagents for alkoxide formation. First, glycerol-1,3-iodohydrin glycerol-1,3-bromohydrin converted into 1,3-methyl- 1,3-ethyl glycerol (98–100%) when reacted with MeOH EtOH, both solvent reagent. A second route employed an source...

We describe in this letter the first enantioselective synthesis of (-)-(2S,6S)-(6-ethyltetrahydropyran-2-yl)formic acid (2) five steps (30% overall yield, 87% ee), from commercial chiral template (R)-2,3-isopropylideneglyceraldehyde (4). The two stereogenic centers 2 were controlled by diastereoselective ­Barbier allylation 4 aqueous media and an efficient Prins ­cyclization reaction between 5 with propanal.

γ-Monosubstituted and trans-α,β-disubstituted γ-lactams were diastereoselectively synthesized from common intermediates (S)-N,N-dibenzylated aldehydes derived natural l-(α)-amino acids, employing a divergent approach. The key features of the routes include diastereoselective Henry Michael reactions that produced chiral γ-nitroester derivatives, which subsequently submitted to tandem reduction-lactamization sequence providing title compounds. versatility can allow preparation several other...

Abstract For see ChemInform in Full Text.

Butyrolactones make part of a class substances with high occurrence in nature. They have different biological profile such as potent antibiotics, antivirals, antifungal among others. Because these important activities various synthetic methodologies capable producing the butyrolactone ring β,γ-disubstituted are available literature, however, few methods allow introduction cis relative stereochemistry between C3-C4 and an acyl group at position C3 . This study aims to develop new route obtain...

Electron deficient nitroalkenes consists of a versatile class compounds reactives in Michael, Friedel- Crafts, Baylis-Hillman, Diels-Alder, Hetero-Diels- Alder, [3+2]-cycloaddition and Cross Coupling reactions. Usually, β-monosubstituted α,β-disubstituted are synthesized via nitroaldol reaction between an aldehyde the nitromethane or primary nitroalkane, respectively. The hydroxyl group elimination, its free active form, leads to desired nitroalkene. Another usual route nitration...