12 results about "Methyl derivative" patented technology

A method of synthesising a 1N-alkyl derivative of pseudouridine comprises contacting a substrate with a methyltransferase in the presence of a cofactor to produce the 1N-alkyl derivative of pseudouridine. The substrate has a structure of: Formula (I). The 1N-methyl derivative of pseudouridine has a structure of: Formula (II). R1 is a hydroxyl group, a monophosphate group, a diphosphate group, or a triphosphate group. R2 is H or a hydroxyl group. R3 is a methyl group or an ethyl group. The cofactor is a source of a methyl group or an ethyl group. The methyltransferase is configured to transfer the methyl group or ethyl group from the cofactor to the substrate. Enzymatic synthesis of 1N-methyl derivatives of pseudouridine may be more efficient and produce less waste than chemical syntheses. Also provided are methyltransferases and buffers useful in the method; and polynucleotides, expression vectors, and microorganisms useful for producing the methyltransferases.

This invention discloses a method for synthesizing medroxyprogesterone acetate intermediates based on a metal-organic synergistic catalysis. The method uses 17-acetyl-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecano-1H-cyclopenta[a]phenanthrene-17-yl acetate as a starting material. Under the synergistic catalytic system composed of a chiral α-amino acid (such as L-proline) and a Lewis acid metal salt (such as zinc acetate), it reacts with a secondary amine and a formaldehyde source to selectively prepare a 6-methylene derivative. This invention utilizes the regio-directing effect of amino acids and the activating and stabilizing effect of metal ions to significantly suppress C2-position side reactions and dimer formation, resulting in a product yield exceeding 93% and a purity exceeding 99%. Column chromatography is not required, making it suitable for large-scale industrial production.

The invention discloses a metallocene catalyst, a preparation method thereof and an application of the metallocene catalyst in olefin polymerization, the preparation method comprises the following steps: (1) adding a raw material 1, a catalyst pentamethylcyclopentadienyl rhodium dimer and a raw material 2 into a first organic solvent, and reacting at 20-100 DEG C for 1-10 hours to obtain an intermediate 1; adding organic amine into the intermediate 1, reacting at 30-100 DEG C for 3-6 hours, filtering, concentrating and recrystallizing to obtain an intermediate 2; the raw material 1 is a Meldrum's acid methylene derivative; the raw material 2 is an acetylene derivative; and (2) adding a second organic solvent into the intermediate 2, adding a strong alkaline substance into the intermediate 2 at-40 to 0 DEG C, stirring and reacting for 1-10 hours, adding halide of M at-20 to 40 DEG C, continuously reacting for 3-24 hours, removing the solvent in vacuum, washing and drying in vacuum. When the catalyst is used for olefin polymerization, the catalytic activity is good, and the molecular weight of the obtained polymer is high.

A method of synthesising a IN-alkyl derivative of pseudouridine comprises contacting a substrate with a methyltransferase in the presence of a cofactor to produce the I N-alkylderivative of pseudourid

The present application relates to a kind of 2-oxazolidinone-3-carbamimidate-5-methylene derivatives and preparation method thereof, belong to organic synthesis technical field.The structure of 2-oxazolidinone-3-carbamimidate-5-methylene derivatives provided in the present application is as shown in formula (I)-(III).2-Oxazolidinone-3-carbamimidate-5-methylene derivatives of the present application can be applied to the synthesis and activity screening of novel oxazolidinone antibiotics, can provide technical support for the further derivatization and biological activity research of 2-oxazolidinone-3-carbamimidate derivative compound, with wide application prospect.

The invention discloses a method for preparing 5-fluorosalicylaldehyde from p-fluorophenol, and belongs to the technical field of organic synthesis. A mild formylation method is realized by innovatively adopting a catalyst and an active methylene derivative (POCl3 + DMF) as a C1 source. According to the method, p-fluorophenol is taken as a raw material, in the presence of a catalytic amount of titanium tetrachloride, p-fluorophenol, phosphorus oxychloride and N, N-dimethylformamide are subjected to Vilsmeier-Haack reaction in dichloromethane to synthesize p-fluorobenzaldehyde, and then a methanol-water recrystallization process is adopted to replace distillation for purification. Core improvements include: (1) titanium tetrachloride catalyzes Vilsmeier-Haack reaction, and by-products are few; (2) the temperature is controlled by stages, and the operation is easy to control; (3) directly dropwise adding reaction liquid to hydrolyze at 10-25 DEG C; and (4) methanol / water recrystallization purification. According to the method, the defects of a traditional process are overcome, the purity of a crude product reaches 85%-92%, the purity after recrystallization is larger than or equal to 98.5%, the yield is stabilized at 88%-91%, and the method is easy and convenient to operate, low in energy consumption, environmentally friendly and easy to industrialize.

Biologically active compounds and their methods of preparation are provided that may be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of non-tumorous indications such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, otorhinolaryngology disorders, ophthalmological or urological disorders. As the compounds exhibit also toxicity against targets (tumor cells, bacteria, inflammation-related cells) without light these biologically active compounds may also be used for the light-independent treatment of such indications. Embodiments also include methods to synthesize boron dipyrromethene complex structures incorporating a substituted 2,3,5,6-tetrafluorophenyl-dipyrromethene (2,3,5,6-tetrafluorophenyldipyrrin) unit or a substituted 3-nitrophenyl-dipyrromethene (3-nitrophenyl-dipyrrin) unit. Amphiphilic compounds with increased anti-tumour and anti-bacterial efficacy are also provided. Specifically, this is achieved by substitution with bromine atoms and sugar moieties.

A method of synthesising a 1N-alkyl derivative of pseudouridine comprises contacting a substrate with a methyltransferase in the presence of a cofactor to produce the 1N-alkyl derivative of pseudouridine. The substrate has a structure of: Formula (I). The 1N-methyl derivative of pseudouridine has a structure of: Formula (II). R1 is a hydroxyl group, a monophosphate group, a diphosphate group, or a triphosphate group. R2 is H or a hydroxyl group. R3 is a methyl group or an ethyl group. The cofactor is a source of a methyl group or an ethyl group. The methyltransferase is configured to transfer the methyl group or ethyl group from the cofactor to the substrate. Enzymatic synthesis of 1N-methyl derivatives of pseudouridine may be more efficient and produce less waste than chemical syntheses. Also provided are methyltransferases and buffers useful in the method; and polynucleotides, expression vectors, and microorganisms useful for producing the methyltransferases.

The present invention concerns aza-metal-dipyrromethene derivatives, processes of production and uses thereof in photocatalysis.

Disclosed are a 3-N-cyclopropylmethyl-2-fluorobenzamide compound, a preparation method therefor and the use thereof. The compound has a structure as represented by the following formula I. This compound can be used for the preparation of an m-diamide compound substituted with a 3-N-cyclopropylmethyl derivative. The m-diamide compound substituted with the 3-N-cyclopropylmethyl derivative, when serving as an insecticide, has the characteristics of a good fast-acting property, needing to use a low amount thereof, and being more beneficial for environmental protection. The 3-N-cyclopropylmethyl-2-fluorobenzamide compound is easy to synthesize and has mild conditions, and when used for preparing a m-diamide compound insecticide substituted with a 3-N-cyclopropylmethyl derivative, same is easy to synthesize and has a low synthesis cost and a high yield.