Tag: M.W=300-350

McDonald, Frank E. published the artcileStereo- and regioselective synthesis of 2-amino-3,5-diols via stereospecific crotyl transfer and regioselective aminohydroxylation, SDS of cas: 99438-28-5, the publication is Synthesis (2012), 44(23), 3639-3648, database is CAplus.

A short synthesis of 2-amino-3,5-diols is described, including the all-S isomer enigmol, a synthetic anticancer compound inspired by the structure of fumonisin B₁. The synthetic route features stereospecific crotyl transfer to tetradecanal via pericyclic oxonia-Cope rearrangement; stereoselective epoxidation of the alkene; regioselective epoxide opening with azide; and reduction of azide to amine. This manuscript also corrects a structure assignment error in a previously reported synthesis of one of the diastereomers of enigmol.

Synthesis published new progress about 99438-28-5. 99438-28-5 belongs to ethers-buliding-blocks, auxiliary class Chiral,Aliphatic cyclic hydrocarbon, name is (+)-B-Methoxydiisopinocampheylborane, and the molecular formula is C21H37BO, SDS of cas: 99438-28-5.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Roush, W. R. published the artcile[(E)-γ-(Dimethylphenylsilyl)allyl]diisopinocampheylborane: a highly enantioselective reagent for the synthesis of anti-β-hydroxyallylsilanes, COA of Formula: C21H37BO, the publication is Tetrahedron Letters (2000), 41(49), 9413-9417, database is CAplus.

Anti-β-Hydroxyallylsilanes, MeCH(OH)CH(CH:CH₂)SiMe₂Ph for example, were prepared with 88-95% e.e. via asym. allylboration reactions of aldehydes, MeCHO for example, with [(E)-γ-(dimethylphenylsilyl)allyl]diisopinocampheylborane.

Tetrahedron Letters published new progress about 99438-28-5. 99438-28-5 belongs to ethers-buliding-blocks, auxiliary class Chiral,Aliphatic cyclic hydrocarbon, name is (+)-B-Methoxydiisopinocampheylborane, and the molecular formula is C21H37BO, COA of Formula: C21H37BO.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Keiser, Jennifer published the artcileEvaluation of an FDA approved library against laboratory models of human intestinal nematode infections, Related Products of ethers-buliding-blocks, the publication is Parasites & Vectors (2016), 376/1-376/10, database is CAplus and MEDLINE.

Background: Treatment options for infections with soil-transmitted helminths (STH) – Ascaris lumbricoides, Trichuris trichiura and the two hookworm species, Ancylostoma duodenale and Necator americanus – are limited despite their considerable global health burden. The aim of the present study was to test the activity of an openly available FDA library against laboratory models of human intestinal nematode infections. Methods: All 1,600 drugs were first screened against Ancylostoma ceylanicum third-stage larvae (L3). Active compounds were scrutinized and toxic compounds, drugs indicated solely for topical use, and already well-studied anthelmintics were excluded. The remaining hit compounds were tested in parallel against Trichuris muris first-stage larvae (L1), Heligmosomoides polygyrus third-stage larvae (L3), and adult stages of the three species in vitro. In vivo studies were performed in the H. polygyrus and T. muris mice models. Results: Fifty-four of the 1,600 compounds tested revealed an activity of > 60% against A. ceylanicum L3 (hit rate of 3.4%), following incubation at 200μM for 72 h. Twelve compounds progressed into further screens. Adult A. ceylanicum were the least affected (1/12 compounds active at 50μM), while eight of the 12 test compounds revealed activity against T. muris L1 (100μM) and adults (50μM), and H. polygyrus L3 (200μM). Trichlorfon was the only compound active against all stages of A. ceylanicum, H. polygyrus and T. muris. In addition, trichlorfon achieved high worm burden reductions of 80.1 and 98.9%, following a single oral dose of 200 mg/kg in the T. muris and H. polygyrus mouse model, resp. Conclusion: Drug screening on the larval stages of intestinal parasitic nematodes is feasible using small libraries and important given the empty drug discovery and development pipeline for STH infections. Differences and commonalities in drug activities across the different STH species and stages were confirmed. Hits identified might serve as a starting point for drug discovery for STH.

Parasites & Vectors published new progress about 637-58-1. 637-58-1 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is 4-(3-(4-Butoxyphenoxy)propyl)morpholine hydrochloride, and the molecular formula is C17H28ClNO3, Related Products of ethers-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Young, Trudye A. published the artcileA pramoxine-based anti-itch lotion is more effective than a control lotion for the treatment of uremic pruritus in adult hemodialysis patients, COA of Formula: C17H28ClNO3, the publication is Journal of Dermatological Treatment (2009), 20(2), 76-81, database is CAplus and MEDLINE.

Objective: The objective of this study was to evaluate the efficacy of a com. available anti-itch lotion containing 1% pramoxine hydrochloride vs. control lotion in the treatment of uremic pruritus in adult hemodialysis patients. Methods: This was a randomized, double-blind, controlled comparative trial set in a community hemodialysis center. The study population comprised 28 individuals (mean age 53.5) with moderate to severe uremic pruritus who had been receiving hemodialysis for at least 3 mo. All participants were recruited from one community hemodialysis center. Topical anti-itch lotion containing 1% pramoxine was applied twice daily to all affected areas of pruritus for 4 wk. The main outcome measure was a reduction in itch intensity. Secondary outcomes included increases in the investigator’s global assessment and improvement in skin hydration. Results: There was a 61% decrease in itch intensity in the treatment group, whereas a 12% reduction in itch intensity was observed in the control group. The rate of decline in itching was also greater in the treatment arm vs. the control arm. No significant differences were displayed in other studied disease-related variables. Conclusion: Our study shows that individuals using pramoxine 1% lotion experienced a reduction in pruritus to a greater degree than those using the control lotion. This safe, convenient and effective topical lotion may potentially benefit the large number of patients affected by pruritus associated with end-stage renal disease.

Journal of Dermatological Treatment published new progress about 637-58-1. 637-58-1 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is 4-(3-(4-Butoxyphenoxy)propyl)morpholine hydrochloride, and the molecular formula is C6H17NO3Si, COA of Formula: C17H28ClNO3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Fuwa, Haruhiko published the artcileTotal Synthesis, Stereochemical Reassignment, and Biological Evaluation of (-)-Lyngbyaloside B, Computed Properties of 99438-28-5, the publication is Angewandte Chemie, International Edition (2015), 54(3), 868-873, database is CAplus and MEDLINE.

(-)-Lyngbyaloside B is a 14-membered macrolide glycoside isolated from the marine cyanobacterium Lyngbya sp. as a cytotoxic substance by Moore and co-workers. The first total synthesis of (-)-lyngbyaloside B and the reassignment of its stereo-structure is described. The synthesis features an Abiko-Masamune aldol reaction, a vinylogous Mukaiyama aldol reaction, and a macrocyclization involving an acyl ketene intermediate for the construction of the macrocyclic backbone, which contains an acylated tertiary alc. The antiproliferative activity of selected compounds against a small panel of human cancer cell lines is also reported.

Angewandte Chemie, International Edition published new progress about 99438-28-5. 99438-28-5 belongs to ethers-buliding-blocks, auxiliary class Chiral,Aliphatic cyclic hydrocarbon, name is (+)-B-Methoxydiisopinocampheylborane, and the molecular formula is C21H37BO, Computed Properties of 99438-28-5.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Smith, Amos B. III published the artcileTotal Syntheses of (-)-Macrolactin A, (+)-Macrolactin E, and (-)-Macrolactinic Acid: An Exercise in Stille Cross-Coupling Chemistry, Recommanded Product: (+)-B-Methoxydiisopinocampheylborane, the publication is Journal of the American Chemical Society (1998), 120(16), 3935-3948, database is CAplus.

The total syntheses of the potent antiviral agent (-)-macrolactin A (I; R¹ = OH, R² = H) and two related family members, (+)-macrolactin E (I; R¹R² = O) and (-)-macrolactinic acid (II; X = CH₂CH₂CH₂), have been achieved, exploiting a unified, convergent, and highly stereocontrolled strategy. Extensive use of the palladium-catalyzed Stille cross-coupling reaction for the stereospecific construction of the three isolated dienes including macrocyclization formed the cornerstone of the successful strategy. The total syntheses of these natural products, no longer available via fermentation, confirm their relative and absolute stereochemistries and provide access to possible analogs for further biol. study.

Journal of the American Chemical Society published new progress about 99438-28-5. 99438-28-5 belongs to ethers-buliding-blocks, auxiliary class Chiral,Aliphatic cyclic hydrocarbon, name is (+)-B-Methoxydiisopinocampheylborane, and the molecular formula is C5H10O, Recommanded Product: (+)-B-Methoxydiisopinocampheylborane.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Wilkes, Sally R. published the artcileHow Clinically Relevant Are Treatment Comparisons of Topical Calcineurin Inhibitor Trials for Atopic Eczema?, COA of Formula: C17H28ClNO3, the publication is Journal of Investigative Dermatology (2016), 136(10), 1944-1949, database is CAplus and MEDLINE.

We sought to explore the architecture of trials of calcineurin inhibitors for atopic eczema to document the extent to which comparisons with active treatments such as topical corticosteroids might have been included or avoided. We identified all eligible randomized controlled trials using the Global Resource for EczemA Trials (GREAT) database. Network plots were produced where the nodes represented a treatment type and the lines between the nodes represented the number of trials or participants involved in the various treatment comparisons. A total of 174 randomized controlled trials for atopic eczema treatments were identified in which pimecrolimus, tacrolimus, or topical corticosteroids were compared with another intervention or a vehicle/emollient. Of 39 trials involving pimecrolimus and 41 trials involving tacrolimus, 8 (20.5%) and 13 (31.7%), resp., made comparisons with topical corticosteroids, and 25 (64.1%) and 15 (36.6%), resp., were vehicle-controlled studies. The high rate of comparisons with vehicle controls in randomized controlled trials that assessed the efficacy of pimecrolimus or tacrolimus long after efficacy had been established is a matter of concern. Active comparators (mild topical corticosteroids for pimecrolimus and moderate to potent topical corticosteroids for tacrolimus) are best placed to determine how topical calcineurin inhibitors compare with established clin. practice.

Journal of Investigative Dermatology published new progress about 637-58-1. 637-58-1 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is 4-(3-(4-Butoxyphenoxy)propyl)morpholine hydrochloride, and the molecular formula is C4H5F3N2O3S, COA of Formula: C17H28ClNO3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Popovic, Radomir published the artcileCoulometric determination of some local anesthetics, COA of Formula: C17H28ClNO3, the publication is Acta Pharmaceutica Jugoslavica (1967), 17(2), 77-80, database is CAplus.

Coulometric determination of the local anesthetics procaine-HCl, tetracaine-HCl, lignocaine-HCl, amylocaine-HCl, dibucaine-HCl, pramoxine-HCl, Panthesine-HCl, and Falicaine-HCl is proposed. After passing the solution (1%) of anesthetic through a column of Dowex 2 the effluent (5 ml.) is titrated coulometrically in the anode compartment in the presence of 10 ml. 0.01 N H2SO4 and 5 drops phenolphthalein.

Acta Pharmaceutica Jugoslavica published new progress about 637-58-1. 637-58-1 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is 4-(3-(4-Butoxyphenoxy)propyl)morpholine hydrochloride, and the molecular formula is C17H28ClNO3, COA of Formula: C17H28ClNO3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Yamauchi, Satoshi published the artcileStereoselective syntheses of cryptocarya diacetate and all its stereoisomers in optically pure forms, Synthetic Route of 99438-28-5, the publication is Bioscience, Biotechnology, and Biochemistry (2015), 79(1), 16-24, database is CAplus and MEDLINE.

Cryptocarya diacetate and each of its stereoisomers were stereoselectively synthesized in 8-16 steps. One of the three chiral carbons was converted from the chiral center of a yeast-reduction product. The other two chiral carbons were constructed by employing stereoselective allylation and syn-and anti-1,3-reductions The enantiomeric excesses of the synthesized cryptocarya diacetate and its stereoisomers were determined to be more than 99%ee using a chiral column.

Bioscience, Biotechnology, and Biochemistry published new progress about 99438-28-5. 99438-28-5 belongs to ethers-buliding-blocks, auxiliary class Chiral,Aliphatic cyclic hydrocarbon, name is (+)-B-Methoxydiisopinocampheylborane, and the molecular formula is C18H14BrNO5S2, Synthetic Route of 99438-28-5.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Fukuda, Hayato published the artcileSynthesis and Structure-Activity Relationship of Vicenistatin, a Cytotoxic 20-Membered Macrolactam Glycoside, Recommanded Product: (+)-B-Methoxydiisopinocampheylborane, the publication is Chemistry – An Asian Journal (2012), 7(12), 2872-2881, S2872/1-S2872/34, database is CAplus and MEDLINE.

We have developed two syntheses of viceniqstatin and its analogs. Our first-generation strategy included the rapid and sequential assembly of the macrocyclic lactam by using an intermol. Horner-Wadsworth-Emmons reaction between the C3-C13 fragment and the C1-C2, C14-C19 fragment, followed by an intramol. Stille coupling reaction. The second-generation strategy utilized a ring-closing metathesis of a hexa-ene intermediate to generate the desired 20-membered macrolactam. This second-generation strategy made it possible to prepare synthetic analogs of vicenistatin, including the C20- and/or C23-demethyl analogs. Evaluation of the cytotoxic effect of these analogs indicated the importance of the fixed conformation of aglycon for determining the biol. activity of the vicenistatins.

Chemistry – An Asian Journal published new progress about 99438-28-5. 99438-28-5 belongs to ethers-buliding-blocks, auxiliary class Chiral,Aliphatic cyclic hydrocarbon, name is (+)-B-Methoxydiisopinocampheylborane, and the molecular formula is C21H37BO, Recommanded Product: (+)-B-Methoxydiisopinocampheylborane.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem