Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Wang, Yumei, once mentioned the application of 2999-46-4, Name is Ethyl 2-isocyanoacetate, molecular formula is C5H7NO2, molecular weight is 113.1146, MDL number is MFCD00000007, category is chiral-nitrogen-ligands. Now introduce a scientific discovery about this category, Computed Properties of C5H7NO2.
Design and preparation of mesoporous silica carriers with chiral structures for drug release differentiation
In this study, twisted rod-like chiral mesoporous silicas (CMSs) with discriminating chiral characteristics (D/L) were designed and biomimetic synthesized by using L- and D-alanine derivatives as templates, and employed as poorly water-soluble chiral drug ibuprofen (IBU) carriers. The morphology and mesoscopic characteristics of CMSs were determined by transmission electron microscope (TEM) and small-angle X-ray scattering (SAXS). Meanwhile, the physicochemical properties of CMSs before and after drug loading were systematically characterized by infrared spectroscopy (IR), nitrogen adsorption, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and induced circular dichroism (ICD). The results suggested that, the CMSs exhibited local chiral characteristics, which were successfully endowed by the alanine-derivative surfactants templates with a reversal of chirality. The crystalline state of IBU was effectively converted to amorphous state after being incorporated into CMSs, and the drug delivery systems shared the chiral characteristic of carriers. Besides, in vitro drug release experiments were respectively performed in simulated gastric fluid (SGF, pH 1) and simulated intestinal fluid (SIF, pH 6.8) medium, and the results demonstrated that both L-CMS and D-CMS could improve the dissolution of IBU in SGF medium, which could be explained by the amorphization of IBU. Particularly, due to the different pore geometry of these two materials, CMSs with different chirality (D/L) could be applied as carriers to accomplish drug release differentiation.
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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
,Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis