Light Fluorous Synthesis

Zhang, Wei

doi:10.1002/9781119288152.ch19

Cited by 5 publications

(4 citation statements)

References 111 publications

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“…This observation indicates that optimizing phase states is becoming a new stage in rational drug development. Regarding excipients, researchers prefer to use non-toxic and low-toxic solvents that align with the principles of "green" chemistry [56,57]. Dissolution is a critical stage in lyophilization, and different solubilizers are frequently used.…”

Section: Discussionmentioning

confidence: 99%

Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization

Taldaev,

Pankov,

Terekhov

et al. 2023

Pharmaceutics

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Bioavailability is an important biopharmaceutical characteristic of active pharmaceutical ingredients (APIs) that is often correlated with their solubility in water. One of the methods of increasing solubility is freeze drying (lyophilization). The article provides a systematic review of studies published from 2012 to 2022 aimed at optimizing the properties of active pharmaceutical ingredients by freeze drying. This review was carried out in accordance with the recommendations of Preferred Reporting Items for Systematic Reviews and Meta-Analysis (PRISMA). In general, 141 modifications of 36 APIs attributed to 12 pharmacological groups were reported in selected publications. To characterize the products of phase modification after lyophilization, a complex of analytical methods was used, including microscopic, thermal, X-ray, and spectral approaches. Solubility and pharmacokinetic parameters were assessed. There is a tendency to increase solubility due to the amorphization of APIs during lyophilization. Thus, the alcohol lyophilizate of dihydroquercetin is “soluble” in water compared to the initial substance belonging to the category “very poorly soluble”. Based on the analysis of the literature, it can be argued that lyophilization is a promising method for optimizing the properties of APIs.

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Section: Discussionmentioning

confidence: 99%

Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization

Taldaev,

Pankov,

Terekhov

et al. 2023

Pharmaceutics

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“…[16] At present, "Green Chemistry" is playing a crucial role in developing synthetic processes that not only use less hazardous chemicals, solvents, and reagents but also lessen their detrimental effects on the environment. [17,18] Using an easily recyclable heterogeneous catalyst in a chemical reaction is well-established green synthetic strategy that is quickly gaining popularity among the researchers. It plays an important role in lowering the harmful effects of long and tedious synthetic procedures on the environment.…”

Section: Introductionmentioning

confidence: 99%

Ecofriendly Synthesis of DHPMs using Copper-based Nano catalysts and Evaluation of Antibacterial Activity

Sharma,

Khatik,

Khandelwal

et al. 2023

Croat. Chem. Acta

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A new catalytic approach has been developed under microwave irradiation for the multicomponent reaction (MCR) of aromatic aldehydes, urea/thiourea and ethylacetoacetate to give corresponding dihydropyrimidinones (DHPMs) by using CuFe2O4/CuO-CeO2 nanoparticles (NPs) as heterogeneous and recyclable catalysts. 3, 4-Dihydropyrimidin-2(1H) ones/thiones are synthesized in higher yields (80-95 %) and short reaction time (8−10 minutes) at 245 Watts. It is applicable for both types of aromatic aldehydes containing EWS as well as EDS. Further, the synthesized compounds were evaluated for antibacterial activity against E. coli, B. subtilis, B. megaterium, and P. vulgaris. Among the compounds tested, ethyl-6-methyl-2-oxo-4-(4-chlorophenyl)-1,2,3,4-tetrahydropyrimidin-5-carboxylate, 4c showed response against B. subtilis, B. megaterium, and P. vulgaris and ethyl-6-methyl-2-oxo-4-(4-fluorophenyl)-1,2,3,4-tetrahydropyrimidin-5-carboxylate, 4h showed -ve response against E. coli, B. subtilis, B. megaterium, and P. vulgaris.

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“…A fluorous tag strategy of varying tag lengths has been successfully developed in fluorous solid phase (F-SP) separation/extraction, asymmetric catalysis, and synthetic applications of biomedicinal , and natural product interests. Therefore, we also sought to append a p -nona-fluoroheptoxy (NFH) tag at the tail of the vanadyl cluster complexes for their real time domain HPLC analyses with quantification (Figure B).…”

Section: Introductionmentioning

confidence: 99%

Metal-Ion Specific Recognition with Amplified Transcription from Subnanometer to Submillimeter or Real-Time Domain by Self-Assembled Vanadyl Quartets

Chen

Weng

2022

Inorg. Chem.

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Vanadyl(V) complexes 1 and 2 bearing a nematic liquid crystal (LC) like a p-heptoxyphenyl group or a fluorous-tag pnonafluoroheptoxyphenyl (NFH) group at the C5 position of the Nsalicylidene template were designed and synthesized. Each complex was subjected to MVO 3 -induced self-assembly to form metal-ion, encapsulated quartet clusters 3-M and 3′-M. The Na + in cluster complex 3-Na or 3′-Na can be readily replaced by Rb + , Ag + , or Hg 2+ in an aqueous layer to form cluster complexes by ion swapping at the H 2 O/CDCl 3 bilayer interface. Selectivity profiles were examined with alkali-metal ions, Ag + , and Hg 2+ through metal-ion competition experiments. The 3′-Na has an exclusive selectivity for Hg 2+ in the presence of Zn 2+ and Cd 2+ . Cluster complexes 3-M were utilized as chiral dopants to nematic LC materials. The effects of the encapsulated metal ions within the alkali family and Ag + on Cano's line widths and helical pitch changes were viewed in wedge cells under a polarized microscope. Their correlations with the ionic radius were identified. The subnano information of the metal ions can thus be asymmetrically amplified to Cano's line spacings of the submilimeter domain. Conversely, the effects of the encapsulated alkali metal ions and Hg 2+ in 3′-M on the interactions of their NFH tails toward fluorous silica gel (FSG) were performed via HPLC analyses. Their retention times became longer as the sizes of encapsulated, alkali metal ions increased. The increasing ion size from Na + to Cs + caused the four lower rim NFH tags of the cluster to be closer due to reduced cone angles. Their interactions among NFH tail groups on FSG became larger, thus leading to distinctive separations with t R from 7.36 to 10.27 min. The retention time difference between 3′-Na and 3′-Hg on HPLC was ∼3.6 min, resulting in discernible separation. The individual ion size differences on the subnano scale can thus be amplified and unambiguously established in the real time domain.

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Light Fluorous Synthesis

Cited by 5 publications

References 111 publications

Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization

Modification of the Physicochemical Properties of Active Pharmaceutical Ingredients via Lyophilization

Ecofriendly Synthesis of DHPMs using Copper-based Nano catalysts and Evaluation of Antibacterial Activity

Metal-Ion Specific Recognition with Amplified Transcription from Subnanometer to Submillimeter or Real-Time Domain by Self-Assembled Vanadyl Quartets

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