15 results about "Dienedione" patented technology

The invention discloses a method for extracting a p-phenylenediamine antioxidant in a liquid sample and application of the p-phenylenediamine antioxidant. The p-phenylenediamine antioxidant comprises N-(1, 2, 4-trimethyl-1, 3-pentanediol) the organic solvent is at least one of N, N '-diphenyl-1, 3-dimethyl butyl)-N'-phenyl p-phenylenediamine, N-cyclohexyl-N '-phenyl p-phenylenediamine, N-isopropyl-N'-phenyl-p-phenylenediamine, N, N '-diphenyl-1, 4-phenylenediamine, N, N'-di-2-naphthyl p-phenylenediamine and 2-((4-methylpentane-2-yl) amino)-5-(phenyl amino) cyclohex-2, 5-diene-1, 4-diketone. According to the method, liquid-liquid extraction which is simple and efficient to operate, low in cost and good in repeatability is adopted as a sample pretreatment method, and is combined with an isotope label method and an ultra-high performance liquid chromatography-tandem mass spectrometry technology, so that separation and qualitative and quantitative detection of six p-phenylenediamine antioxidants and quinone derivatives in a sample are realized; meanwhile, the sensitivity is high, the quantity of isotope internal standards is small, the solvent loss is small, and the actual detection requirement is met.

The invention discloses a 3-ketosteroid-delta1-dehydrogenase mutant and application of the 3-ketosteroid-delta1-dehydrogenase mutant in catalyzing dehydrogenation of a steroid compound, the mutant with high catalytic activity is obtained through screening, and the solubility of a substrate is increased by adding a cosolvent Tween-80, so that the biological catalytic efficiency is improved. Under the optimal condition, the mutant disclosed by the invention can improve the feeding amount conversion rate of 15g / L of (16 alpha)-methyl androstane-4, 9-diene-3, 17-diketone to 99.9%.

The application discloses a steroid C14 alpha hydroxylase CLCYP14 mutant, relates to the field of proteins, and applies a site-directed saturation mutation technology and a combination mutation strategy to screen and obtain CLCYP14 mutants I111L-M115K and I111L-V124W with high hydroxylation specificity. Compared with CLCYP14, the hydroxylation selectivity and conversion rate of I111L-M115K and I111L-V124W for steroid compounds progesterone, 21-hydroxyprogesterone, 5beta-hydroxyprogesterone, 1-dehydroprogesterone, 21-hydroxypregna-1,4-diene-3,20-dione and deoxycortisone are obviously improved.

The invention discloses a preparation method of deflazacort, which is characterized in that 3-(hydrazinoformyl) hydrazone-16beta, 17beta-epoxy imino-1, 4-pregnadiene-11, 20-diketone is used as a raw material, high-selectivity synthesis of 11beta-hydroxyl is realized at-10 + / -2 DEG C through photocatalysis and steric hindrance-directed reduction of diisopinopinyl borane, and ee (enantiomeric excess) value is greater than or equal to 95%. The preparation method comprises the following steps: after iodinating with N-iodosuccinimide, quenching with sodium thiosulfate, carrying out ring-opening esterification with potassium acetate, and recrystallizing to obtain the product, the total yield is 57%, the impurity content is low, and the preparation method is suitable for industrialization.

The invention relates to the technical field of medicines, and discloses a curcumin derivative and a preparation method thereof, and a nano-composite and a preparation method and application thereof. Wherein the curcumin derivative is (1E, 6E)-1, 7-bis (3, 4-dihydroxyphenyl)-1, 6-heptadiene-3, 5-diketone, and the preparation method of the curcumin derivative comprises the step of carrying out double demethylation treatment on curcumin. The nano-composite contains a chelate of a curcumin derivative and Cu (II). The nano-composite can specifically react with GSH in cancer cells, simultaneously trigger a Fenton reaction and a Michael addition reaction and inhibit GSH synthesis to induce cell apoptosis, consumption of a large amount of GSH further promotes lipid peroxidation (LPO) to trigger ferroptosis, mitochondria can be attacked to cause dysfunction to induce ferroptosis, and in addition, the nano-composite also has good biological safety and can be used for preparing a medicine for treating cancer cells. The compound has a wide prospect in the application of drugs for resisting the drug resistance of cancer cells.

This invention provides a curcumin analogue, its preparation method, and its application, belonging to the field of biomedical technology. The curcumin analogue includes 1,7-bis(3-hydroxy-4-methoxyphenyl)-4-n-butyl-1,6-heptadien-3,5-dione, 1,7-bis(3-hydroxy-4-methoxyphenyl)-4-cyclopropylmethyl-1,6-heptadien-3,5-dione, and 1,7-bis(3-trifluoromethoxyphenyl)-4-n-butyl-1,6-heptadien-3,5-dione. The curcumin analogue provided by this invention can effectively inhibit renal fibrosis, with a significantly better therapeutic effect than curcumin alone, and has potential application value in the field of renal fibrosis treatment drugs.

The invention relates to the field of preparation of steroid drugs, and discloses a preparation method of didrogesterone. The preparation method disclosed by the invention comprises the following steps: by taking 9beta, 10alpha-pregna-4, 7-diene-3, 20-diketone as a starting material, carrying out intramolecular 7, 8-double bond transposition in the presence of organic silicon Lewis acid, so as to obtain the didrogesterone. The preparation method of the didrogesterone, provided by the embodiment of the invention, has the beneficial effects that (1) the purity of a refined product can reach 99% or above, the impurity content is controllable, and the total yield can be increased to 85% or above; reaction conditions are mild, operation is simple, and the method is suitable for industrial production.

The application discloses a 3-steroid ketone-delta 1-dehydrogenase mutant and application thereof in catalyzing dehydrogenation of a steroid compound, and the mutant with high catalytic activity is screened, and a cosolvent Tween-80 is added to increase solubility of a substrate and then improve biological catalytic efficiency.Under optimal conditions, the mutant can increase the conversion rate of (16alpha)-methyl androst-4,9-diene-3,17-dione 15g / L to 99.9%.

The invention provides an improved method for preparing an exemestane intermediate 6-hydroxymethyl-androstane-1, 4-diene-3, 17-diketone, and particularly relates to a method for preparing the 6-hydroxymethyl-androstane-1, 4-diene-3, 17-diketone through a reaction of 1, 3-ditetrahydropyrrolyl-androstane-3, 5-diene-17-ketone under the action of phenol and a formaldehyde aqueous solution, and particularly relates to a method for preparing the 6-hydroxymethyl-androstane-1, 4-diene-3, 17-diketone through the reaction of 1, 3-ditetrahydropyrrolyl-androstane-3, 5-diene-17-ketone. Compared with the prior art, the method has the advantages that the generation of a large amount of bis-hydroxymethylation impurities is avoided, the purity and the yield are improved, the cost is reduced, the stability of the process is improved, and industrialization is facilitated.

The invention discloses a method for jointly degrading 2-((4-methylpent-2-yl) amino)-5-(phenyl amino) cyclohex-2, 5-diene-1, 4-diketone by laccase and a mediator, and belongs to the technical field of environmental organic pollutant treatment.The specific method comprises the steps that mother liquor of pollutants is added into a conical flask, and after acetonitrile volatilizes, the mother liquor of the pollutants is added into the conical flask; the method comprises the following steps: adding a laccase ABTS mediator solution formed by mixing ABTS and laccase to form a reaction system with the pH value of 6.0, reacting at the constant temperature of 40 DEG C for 120 hours, extracting the pollutant by utilizing dichloromethane to terminate the reaction, and determining the residual concentration of the pollutant in the reaction system by adopting an ultra-high performance liquid chromatography so as to analyze the degradation effect of the pollutant. According to the method, a laccase ABTS mediator reaction system is constructed and used for degrading the pollutant 2-((4-methylpent-2-yl) amino)-5-(phenyl amino) cyclohex-2, 5-diene-1, 4-diketone, so that the degradation rate of the pollutant with the initial concentration of 1.0 mg / L reaches 80% or above, and an efficient method is provided for degrading the pollutant in the environment.

The present application relates to an aldehyde mutarotase gene salA and its application in constructing a high-ADD-producing genetically engineered mycobacterium, and a high-ADD-producing genetically engineered mycobacterium and its construction and application in preparing 1,4-androstadiene-3,17-dione by microbial fermentation. The high-ADD-producing genetically engineered mycobacterium is obtained by knocking out kshA1, MnOpccR and salA genes in turn using mycobacterium as a chassis. The genetically engineered strain provided by the present application effectively controls the generation of by-products, greatly improves the utilization rate of steroidal substrates and the molar conversion rate of products, simplifies the post-processing process, and the strategy can also be applied to the synthesis of products in the common synthesis path of 1,4-androstadiene-3,17-dione and 9-OH-AD, which is microbial transformation of side chain degradation using phytosterol as a substrate, completely blocks the synthesis of 4-HBC and 1,4-HBC by-products, and reduces the burden of downstream separation while improving the utilization rate of phytosterol substrate. The present application has certain universality, is suitable for vigorous popularization and application, and has high economic and social benefits.

Derivatives, including deuterated derivatives, of the SHP-1 inhibitor compound 2-(2,5- dichlorophenyl)benzoquinone (which is also referred to as 2-(2,5-dichlorophenyl)cyclohexa-2,5- diene- 1,4-dione, Tyrosine Phosphatase Inhibitor 1 or TPI-1; CAS Registry No. 79756-69-7) are provided. The TPI-1 derivatives can be used in treatment of diseases such as cancer.

Derivatives, including deuterated derivatives, of the SHP-1 inhibitor compound 2-(2,5- dichlorophenyl)benzoquinone (which is also referred to as 2-(2,5-dichlorophenyl)cyclohexa-2,5- diene- 1,4-dione, Tyrosine Phosphatase Inhibitor 1 or TPI-1; CAS Registry No. 79756-69-7) are provided. The TPI-1 derivatives can be used in treatment of diseases such as cancer.

The application belongs to the technical field of biocatalytic synthesis of steroid drugs, and particularly relates to a dehydrogenase, a gene, an engineering bacterium and application, the amino acid sequence of the dehydrogenase is SEQ ID NO. 1 or SEQ ID NO. 2, the dehydrogenase has high dehydrogenation activity, high stereoselectivity and strong regioselectivity, and no other conformation impurities are generated; the engineering bacterium can efficiently secrete the dehydrogenase, and effectively improves the conversion efficiency of a substrate, especially for a substrate 6-methy format (11beta, 17alpha-dihydroxy-6alpha-methylpregna-1, 4-diene-3, 20-diketone), which is low in cost and has significant industrialization potential; the dehydrogenase mutant has clear physicochemical properties, and the method of whole cell catalysis is used, so that the cumbersome step of enzyme purification is omitted, and the cost is reduced and the operation is simple.