Heterocyclic Building Blocks-Benzoxazole

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

In this study, the effect of starch-based and gelatine-based edible coating containing cinnamon oil on selected quality parameters and the metabolism of antioxidants in highbush blueberry fruit, in terms of extending their shelf life were investigated. Research showed that the application of cinnamon oil to edible coating pos. influenced the quality of the fruit during storage. Coating with essential oil effectively inhibited the growth of yeast and mold in the fruit during storage. On the last day, the growth of yeast and mold in the fruit coated with cinnamon oil (10% COE) was 1.29 log cycles lower than in the control. Moreover, the essential oil reduced the loss of soluble solids but it did not significantly affect the acidity and weight loss of the fruit. Equally interesting was the effect of the coating with cinnamon oil on the antioxidant activity of the fruit. Blueberries coated with cinnamon oil were characterised by a lower ability to produce ROS, as well as a lower activity of antioxidant enzymes. On the final day, the level of ROS and the activity of SOD and CAT were lower than the control by 82%, 56% and 63% resp. The level of polyphenols in the fruit coated with cinnamon oil was higher than in the control up to the 5th day of storage. However, the level of anthocyanins in this sample gradually decreased as the storage period extended. After 10 days, the loss of anthocyanins in the fruit with essential oil was around 37%.

Quality and antioxidant activity of highbush blueberry fruit coated with starch-based and gelatine-based film enriched with cinnamon oil. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Iminotetrahydrothiophene 1-oxide (BD00963737) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

An efficient copper-catalyzed C-H/N-H bond functionalization for the synthesis ¦Á-keto-N-acyl sulfoximines from aryl Me ketones and NH-sulfoximines with mol. oxygen as terminal oxidant has been developed. E.g., under an atm. of dioxygen, CuBr in DMSO catalyzed the reaction of PhCOMe and PhSMe(O)(:NH) to give 74% PhCOCON:SMePh(O).

Copper-Catalyzed Oxidative ¦Á-Ketoacylations of Sulfoximines with Aryl Methyl Ketones and Dioxygen as Terminal Oxidant. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Iminotetrahydrothiophene 1-oxide (BD00963737) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

An iron-catalyzed dealkylative acylation of N-alkylsulfoximines RN=S(O)R1R2 [R = CH3, CH3(CH2)3, (CH2)9CH=CH, etc.; R1 = CH3, C6H5, 4-ClC6H4, 4-BrC6H4, 4-H3COC6H4; R2 = CH3, C6H5, c-C3H5; R1R2 = -(CH2)4-] has been developed. This process involves a Polonovski-type dealkylation of an N-alkylated sulfoximine to afford a reactive intermediate that is trapped in the presence of a suitable aldehyde R3CHO (R3 = C6H5, 2-H3CC6H4, 3-ClC6H4, etc.) or anhydride R4C(O)OC(O)R4 [R = CH3, CH3(CH2)4, C6H5CH=CH, etc.] to afford N-acylsulfoximine derivatives R1R2S(O)=NR4 and N-aroylsulfoximine derivatives R1R2S(O)=NR3 in one pot. Subsequent cleavage of the acyl or aroyl group under acidic conditions generates a synthetically valuable NH-sulfoximines R1R2S(O)=NH.

Iron-Catalyzed Acylative Dealkylation of N-Alkylsulfoximines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

Varroosis is a disease caused by the mite Varroa destructor, and it is considered one of the biggest threats to honey bee populations globally. Mite control is centered on the use of synthetic acaricides, such as amitraz and flumethrine. However, high usage of these chems. is associated with a wide variety of undesirable effects on bee colonies, including the development of resistance and persistence of harmful residues of acaricides in hive products used by humans. Botanical extracts have been identified as a potentially suitable organic alternative to synthetic acaricides. Essential oils, such as clove, eucalyptus, lemongrass, and oregano, have been found to exhibit acaricidal activity against V. destructor. The main goal of this work was to assess the bioactivity of the Cymbopogon nardus essential oil from two different locations (Argentina and India), and the activity of its major component the monoterpene citronellal. According to our results, complete essential oil from India is more effective in controlling parasitosis than the isolated citronellal component. The essential oil of C. nardus from Argentina demonstrated promise for the control of varroosis, as well as exhibiting low toxicity against bees (LC50 = 11.84 ¦ÌL/mL). In addition, this essential oil may avoid the problems caused by synthetic acaricides, such as the emergence of resistance foci in Varroa and residues in hive products. Future research needs to investigate the delivery of volatile essentials oils to target mite populations.

Lethal concentrations of Cymbopogon nardus essential oils and their main component citronellal on Varroa destructor and Apis mellifera. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

2,3-Cl2C6H3NH2 (20 g.) added dropwise to 120 cc. ClSO3H, the mixture heated 48 hrs. at 110¡ã, cooled, poured onto ice, filtered, the residue added in small portions to liquid NH3, the NH3 evaporated, the residue dissolved twice in hot dilute NH4OH, and reprecipitated with AcOH gave 10.8 g. 6,5,4,1,3-Cl2(H2N)C6H(SO2NH2)2, m. 293-4¡ã. 2,5-Cl2C6H3NH2 (I) (10 g.) in 60 cc. ClSO3H heated 4 hrs. at 125¡ã, hydrolyzed, and treated in the usual manner with NH3 yielded 7.8 g. 5,2,4,1,3-Cl2(H2N)C6H(SO2NH2)2, needles, m. 258-9¡ã (EtOH). A similar run at 170¡ã during 0.5 hr. gave the monosulfonamide (II) of I, which refluxed 2 hrs. in ClSO3H, hydrolyzed, and treated with NH3 did not give a pure product. II (5.8 g.), 1.0 g. 5% Pd-C, 20 cc. 5N NaOH, and 100 cc. H2O hydrogenated 15 min. at 2 atm., filtered, and acidified gave 12.5 g. 4,6,2-Cl2(H2N)C6H2SO2NH2 (III), needles, m. 162-2¡ã (H2O). III refluxed 4 hrs. in ClSO3H and treated with NH3 gave a small amount of a mixture of III and the desired disulfonamide. III (5.7 g.) dehalogenated catalytically in the usual manner yielded 2.35 g. o-H2NC6H4SO2NH2, m. 153-4.5¡ã. 3,4-Cl2C6H3NH2 (10 g.) in 60 cc. ClSO3H heated 4 hrs. at 125¡ã, hydrolyzed, and treated with NH3 in the usual manner gave 5.5 g. 4,5,2-Cl2(H2N)C6H2SO2NH2, m. 175.5-6.5¡ã (aqueous Me2CO). 4,2-Cl(O2N)C6H3SO2NH2 (19 g.) in EtOH hydrogenated at low pressure over Pd-C gave 12.2 g. 4,2-Cl(H2N)C6H3SO2NH2, m. 144-6¡ã. The appropriate sulfonamide in 98% HCO2H refluxed 2 hrs., poured into H2O, and filtered gave 73-94% of the corresponding 1,2,4-benzothiadiazine 1,1-dioxide (IV); in this manner were prepared the following compounds (m.p. given): IV, 221-2¡ã (iso-PrOH); 5,6-dichloro-7-sulfamoyl derivative (V) of I, 314-15¡ã; 6,8-di-Cl derivative (VI) of I, 309-10¡ã; 6,7,-di-Cl derivative (VII) of I, 310-11¡ã (iso-PrOH); 6-Cl derivative (VIII) of I, 255-6¡ã. The appropriate sulfonamide in H2O, Me2CO, or aqueous Me2CO containing formalin refluxed 2 hrs., cooled (when Me2CO was used, diluted with H2O), and filtered gave 83-97% of the corresponding 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide; in this manner were prepared the 3,4-dihydro derivatives of the following compounds (m.p. given): V, 302-3¡ã; VI, 249-50¡ã; VII, 207-9¡ã; IV, 171-2¡ã (H2O or iso-PrOH); VIII, 172-3¡ã. V was slightly more potent than chlorothiazide (IX). Dihydro derivative of V was more active as a diuretic than IX, but not as active as dihydro derivative of IX.

Synthesis of potential diuretic agents. II. Dichloro derivatives of 1,2,4-benzothiadiazine 1,1-dioxide. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Iminotetrahydrothiophene 1-oxide (BD00963737) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A new series of 4-alkyl(aryl)-4-tetramethylenesulfoximide-1,1,1-trifluoroalk-3-en-2-ones was prepared from the O,N-exchange reactions of 4-alkyl(aryl)-4-alkoxy-1,1,1-trifluoroalk-3-en-2-ones with the cyclic S,S-tetramethylenesulfoximide in absence of solvent, in good yields. Subsequently, the easy preparation of a new series of a fused heterocyclic system of 3-aryl-5-trifluoromethyl-7,8-dihydro-6H-thieno[2,1-f][1,2]thiazine 1-oxide derivatives (60-85% yields) from intramol. cyclization reactions of sulfoximide enones employing potassium t-butoxide in di-Et ether at reflux was also reported.

An easy approach to the synthesis of new fused 3-aryl-5-trifluoromethyl-7,8-dihydro-6H-thieno[2,1-f][1,2]thiazine 1-oxide system. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

Phytochems. are toxic to insects, but their insecticidal efficiencies are usually low compared to synthetic insecticides. Understanding the mechanism of insect adaptation to phytochems. will provide guidance for increasing their efficacy. We found that exposure to 0.5% indole-3-methanol (I3C), xanthotoxin, and rotenone (ROT) significantly retarded the growth of Spodoptera litura larvae. The oxidative stress in S. litura larvae exposed to phytochems. was increased. The up-regulation of glutamate cysteine ligase but not glutathione reductase revealed that the de novo synthesis pathway is responsible for GSH synthesis in phytochem.-treated larvae. Treatment with the inhibitor (BSO) of ¦Ã-glutamylcysteine synthetase (gclc), a subunit of glutamate cysteine ligase, resulted in decreases of GSH levels and GST activities, increases of ROS levels in I3C-treated larvae, which finally caused midgut necrosis and larval death. Treatment with BSO or I3C alone did not cause larval death. The addition of GSH could partly reduce the influence of I3C and BSO on S. litura growth. Nilaparvata lugens gclc RNAi confirmed the result of BSO treatment in S. litura. N. lugens gclc RNAi significantly increased the mortality of ROT-sprayed N. lugens, in which ROS levels were significantly increased. All data indicate that gclc is involved in insect response to phytochem. treatment. Treatment with dsgclc will increase the insecticidal efficacy of plant-derived compounds

Inhibition of the glutathione biosynthetic pathway increases phytochemical toxicity to Spodoptera litura and Nilaparvata lugens. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

Herein, we report a simple and metal-free method for the synthesis of N-azine sulfoximines by the nucleophilic substitution of azine N-oxides with NH-sulfoximines. The present method works at room temperature with wide functional group compatibility and gives several unprecedented N-azine sulfoximines. The reaction conditions were also found suitable with enantiopure substrates and furnished products without any racemization. It also finds an application in the sulfoximination of azine-based functional mols. such as 2,2′-bipyridine, 1,10-phenanthroline, and quinine.

Metal-Free, Phosphonium Salt-Mediated Sulfoximination of Azine N-Oxides: Approach for the Synthesis of N-Azine Sulfoximines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

4-(S-Methylsulfonimidoyl)benzonitrile (BD00975057) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

Mechanochem. N-sulfenylations of sulfoximines and sulfonimidamides mediated by silver oxide under solvent-free conditions has been developed. The reactions are easy to perform and proceed well on a gram scale. A wide range of functional groups in the substrates were tolerated. Compared to its solvent-based counterpart, the mechanochem. approach showed significant ecol. advantages.

Mechanochemical Solvent-Free N-Sulfenylations of Sulfoximines and Sulfonimidamides. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

Excess generation of reactive oxygen species (ROS) based on sensitizers under ultrasound (US) excitation can cause the death of tumor cells via oxidative damage, but sonosensitizers are largely unexplored. Herein, oxygen-deficient black BiOCl (B-BiOCl) nanoplates (NPs) are reported, with post-treatment on conventional BiOCl by simple UV excitation, showing stronger singlet oxygen (1O2) generation than com. TiO2 nanoparticles and their derivatives under US irradiation. Moreover, L-buthionine-sulfoximine (BSO), a GSH biosynthesis inhibitor, is incorporated into B-BiOCl NPs. The authors find that BSO can be released owing to the degradation of B-BiOCl NPs in the presence of acid and GSH, which are overexpressed in tumors. The results show that BSO/B-BiOCl-PEG NPs have a multifunctional synergistic effect on improving ROS production. In particular, BiOCl has remarkable near-IR light absorption after UV treatment and is good for photoacoustic imaging that can guide subsequent sonodynamic therapy. This work shows that just with a simple oxygen deficiency treatment, strong 1O2 generation can be provided to a conventional material under US irradiation and, interestingly, this effect can be amplified by using a small inhibitor BSO, and this is clearly demonstrated in cell and mice experiments

Oxygen-Deficient BiOCl Combined with L-Buthionine-Sulfoximine Synergistically Suppresses Tumor Growth through Enhanced Singlet Oxygen Generation under Ultrasound Irradiation. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem