6 research outputs found
Lipase-Catalyzed Domino Michael-Aldol Reaction of 2-Methyl-1,3-Cycloalkanedione and Methyl Vinyl Ketone for the Synthesis of Bicyclic Compounds
<div><p></p><p>Synthesis of bicyclic compounds was achieved via a lipase-catalysed, stereoselective, domino Michael-aldol reaction of 2-methyl-1,3-cycloalkanedione and methyl vinyl ketone. Appropriate reaction conditions, including the type of enzyme, solvent, and temperature, were determined. In addition, the effects of solvent polarity and addtives were investigated. The reaction proceeded in the presence of lipase AS in a solution of 20% acetone in dimethylsulfoxide (DMSO) at 10 °C for 8 days, followed by the addition of <i>p</i>-toluenesulfonic acid (TsOH) to afford bicyclic compounds in 51%–83% yields with moderate stereoselectivity. Although this domino Michael-aldol reaction showed only moderate stereoselectivity, even with the acid-supported enhancement of the reaction, these results represent potential new applications for lipase.</p></div
Additional file 1: of GWAS-identified CCR1 and IL10 loci contribute to M1 macrophage-predominant inflammation in Behçet’s disease
Figure S1. Comparison of phenotypic features and cytokine profiles between M1 and M2 cultured cells. Figure S2. eQTL effect of rs7616215 on CCR2 and CCR1. Figure S3. Detailed results of chemotaxis of M2 Mφ toward various concentrations of MIP-1α. Figure S4. Differences in CCR1 positivity (fluorescence-activated cell sorting) between treatments. a Biologics. b Colchicine. c Prednisolone. Figure S5. The number of differentiated Mφ in vitro in HC and BD. Figure S6. eQTL effect of rs1518111 on IL-10 protein and mRNA. Figure S7. Schema showing our proposed immunological responses in BD. Table S1. Characteristics of patients with BD who participated in the study. Table S2. Characteristics of HC study participants. (DOCX 9663 kb
Enantioselective Diels–Alder Reaction of 1,2-Dihydropyridines with Aldehydes Using β‑Amino Alcohol Organocatalyst
The
enantioselective Diels–Alder reaction of 1,2-dihydropyridines
with aldehydes using an easily prepared optically active β-amino
alcohol catalyst was found to provide optically active isoquinuclidines,
an efficient synthetic intermediate of pharmaceutically important
compounds such as oseltamivir phosphate, with a satisfactory chemical
yield and enantioselectivity (up to 96%, up to 98% ee). In addition,
the obtained highly optically pure isoquinuclidine was easily converted
to an optically active piperidine having four successive carbon centers
Enantioselective Diels–Alder Reaction of 1,2-Dihydropyridines with Aldehydes Using β‑Amino Alcohol Organocatalyst
The
enantioselective Diels–Alder reaction of 1,2-dihydropyridines
with aldehydes using an easily prepared optically active β-amino
alcohol catalyst was found to provide optically active isoquinuclidines,
an efficient synthetic intermediate of pharmaceutically important
compounds such as oseltamivir phosphate, with a satisfactory chemical
yield and enantioselectivity (up to 96%, up to 98% ee). In addition,
the obtained highly optically pure isoquinuclidine was easily converted
to an optically active piperidine having four successive carbon centers
Additional file 1: of Dysregulated heme oxygenase-1low M2-like macrophages augment lupus nephritis via Bach1 induced by type I interferons
Table S1. Primer sequences used for qRT-PCR. Figure S1. Numbers of CD68, CD163, HO-1 positive cells in the glomerulus of lupus nephritis patients (ClassI or II). Figure S2. Numbers of CD68, CD163, HO-1 positive cells in the extra-glomerulus of lupus nephritis patients. Figure S3. HO-1 mRNA expression in M1 and M2 Mϕ stimulated with various regents. Figure S4. Genomic background of congenic mice. Figure S5. Genotyping of Bach1 knockout mice. (DOCX 953 kb
Additional file 2: Table S2. of The predictive prognostic factors for polymyositis/dermatomyositis-associated interstitial lung disease
Comparison of demographic data among each PM/DM subtype in PM/DM-ILD patients. (PDF 102 kb