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The process involves ring opening and ring closure of compounds containing a tetrahydrofuroyl group STR1 to provide facile synthesis of compounds containing a piperidin-2-one group of the formula STR2

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Synergism in catalytic activity with the combined use of Hf(O-i-Pr) 4 or Zr(O-i-Pr)4 and Fe(O-i-Pr)3 for direct esterification and a very simple method for their extraction with ionic liquids for their recovery and reuse are described. This Zr(IV)-Fe(III) complex is an environmentally benign catalyst due to its high turnover number, extremely mild Lewis acidity, low toxicity, reusability, and commercial availability at low cost.

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Significance: It is increasingly clear that proline metabolism plays an important role in metabolic reprogramming, not only in cancer but also in related fields such as aging, senescence, and development. Although first focused on proline catabolism, recent studies from a number of laboratories have emphasized the regulatory effects of proline synthesis and proline cycling. Recent Advances: Although proline dehydrogenase/proline oxidase (PRODH/POX) has been known as a tumor protein 53 (P53)-activated source of redox signaling for initiating apoptosis and autophagy, senescence has been added to the responses. On the biosynthetic side, two well-recognized oncogenes, c-MYC and phosphoinositide 3-kinase (PI3K), markedly upregulate enzymes of proline synthesis; mechanisms affected include augmented redox cycling and maintenance of pyridine nucleotides. The reprogramming has been shown to shift in clonogenesis and/or metastasis. Critical Issues: Although PRODH/POX generates reactive oxygen species (ROS) for signaling, the cellular endpoint is variable and dependent on metabolic context; the switches for these responses remain unknown. On the synthetic side, the enzymes require more complete characterization in various cancers, and demonstration of coupling of proline metabolites to other pathways may require studies of protein-protein interactions, membrane transporters, and shuttles. Future Directions: The proline metabolic axis can serve as a scaffold on which a variety of regulatory mechanisms are integrated. Once understood as a central mechanism in cancer metabolism, proline metabolism may be a good target for adjunctive cancer therapy.

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A series of substituted (alpha-alkylidene)tetrahydrofurans was prepared by tungsten catalyzed reaction of substituted hydroxyfuroic acids.These reactions likely involve beta-lactone intermediates which decarboxylate under the reaction conditions, and rates for olefin synthesis correlated with donor properties of substituents at C(4).

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New Advances in Chemical Research, May 2021.Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. HPLC of Formula: C15H19NO4, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 166591-85-1, name is 2-(tert-Butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid. In an article,Which mentioned a new discovery about 166591-85-1

The invention relates to a process for the preparation of alfuzosin hydrochloride method, method comprises the following steps: (1) 15 C following, acrylonitrile into the the methylamine is mellow solution to stir, by distillation to obtain (I); (2) to (I) is dripped reducing agent in an organic solvent, heating to reflux, then slowly sequentially into the 25% sodium hydroxide solution and distilled water, by the distillation treatment to obtain the (II); (3) under dry condition, the thionyl chloride is slowly dripped into the 2 – tetrahydrofuran formic acid, a 2 – tetrahydrofuran chloride; (4) the temperature control in the 5 – 15 C conditions, will be 2 – tetrahydrofuran formyl the chlorine drips into containing acid, organic solvent and (II) of the mixed solution, then completing the stirring 3 hours, for 25% sodium hydroxide solution to neutralize, by organic solvent extraction, (III) be; (5) to (III) with 2 – chloro – 4 – amino – 6, 7 – dimethoxy quinazoline in presence of organic solvent, reflux stirring 4 – 10 hours, cooling and filtering, and steaming and removing the organic solvent, acetone dispersed precipitate solid, then re-crystallizing mixed solvent, to get the alfuzosin hydrochloride (IV). (by machine translation)

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Selective hydrodeoxygenation of 2-furancarboxylic acid, which can be a relatively stable platform chemical from hemicellulose, to valeric acid was investigated in detail, and the reaction has been reported to be specifically promoted by supported Pt-MoOx catalysts. The dependence of catalytic performance of Pt-MoOx/TiO2 on loading amounts of Pt and Mo showed that the highest activity is obtained at around Mo ?0.5 wt % when the Pt loading amount is fixed. With enough of the catalyst that can minimize the effect of deactivation, ?60% yield of valeric acid was obtained over all Pt-MoOx/TiO2 catalysts with Pt ? 1 wt % and 0.5 wt % Mo loadings. Characterization results of Pt-MoOx/TiO2 catalysts with XRD and CO adsorption showed that the Pt particles (3-5 nm, depending on Pt loading amount) were not covered with MoOx species, suggesting that MoOx species were mainly located on the TiO2 support surface. Mo K-edge XAFS results suggest that the MoOx species in Pt-MoOx/TiO2 have a Mo(IV) valence state and some of the MoIVOx species have direct bonds with the Pt atom on Pt metal particles. The number of the direct Pt-Mo bonds became smaller after catalytic use, which can be related to the deactivation. Therefore, the Pt-Mo bimetallic site can be the catalytically active site. Based on the solvent effect, reactivity trends of related substrates, and reaction orders in kinetics, a reaction mechanism is proposed where the ring is opened after addition of one hydrogen atom to the 2-position of the furan ring.

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The discovery and pharmacological evaluation of potent, selective, and orally bioavailable growth hormone secretagogue receptor (GHS-R) antagonists are reported. Previously, 2,4-diaminopyrimidine-based GHS-R antagonists reported from our laboratories have been shown to be dihydrofolate reductase (DHFR) inhibitors. By comparing the X-ray crystal structure of DHFR docked with our GHS-R antagonists and GHS-R modeling, we designed and synthesized a series of potent and DHFR selective GHS-R antagonists with good pharmacokinetic (PK) profiles. An amide derivative 13d (Ca2+ flux IC50 = 188 nM, [brain]/[plasma] = 0.97 @ 8 h in rat) showed a 10% decrease in 24 h food intake in rats, and over 5% body weight reduction after 14-day oral treatment in diet-induced obese (DIO) mice. In comparison, a urea derivative 14c (Ca 2+ flux IC50 = 7 nM, [brain]/[plasma] = 0.0 in DIO) failed to show significant effect on food intake in the acute feeding DIO model. These observations demonstrated for the first time that peripheral GHS-R blockage with small molecule GHS-R antagonists might not be sufficient for suppressing appetite and inducing body weight reduction.

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1-(4-(9H-Carbazol-9-yl)phenyl)-3-amino-9H-fluorene-2,4-dicarbonitrile as a new photocatalyst for the decarboxylative cross-coupling reaction of alpha-amino acids or alpha-oxy carboxylic acids with arylnitriles is described. This light-driven reaction enables a variety of benzylic amines and ethers to be prepared from readily available starting materials under mild conditions.

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alpha-Amino acids are among the most common biologically active molecules in nature, and their functionalization has attracted much attention. In this communication, a novel, efficient and general visible-light photocatalytic decarboxylative monofluoroalkenylation of N-protected alpha-amino acids with gem-difluoroalkenes is reported, affording the corresponding alpha-amino monofluoroalkenes which might find applications in medical chemistry and materials science. The reaction proceeded at room temperature with high efficiency and tolerance of various functional groups.

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The invention relates to processes for the preparation of alfuzosin or pharmaceutically acceptable salts thereof in high purity. More particularly, it relates to the preparation of pure crystalline alfuzosin base. The invention also relates to pharmaceutical compositions that include the pure alfuzosin or a pharmaceutically acceptable salt thereof.

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