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635 results about "Reductive amination" patented technology

Reductive amination (also known as reductive alkylation) is a form of amination that involves the conversion of a carbonyl group to an amine via an intermediate imine. The carbonyl group is most commonly a ketone or an aldehyde. It is considered the most important way to make amines, and a majority of amines made in the pharmaceutical industry are made this way.

Nitrogen-doped carbon material supporting cobalt catalyst and method therewith of catalytic hydrogenation reductive amination to produce amine compounds

The invention discloses a nitrogen-doped carbon material supporting cobalt catalyst and a method therewith of catalytic hydrogenation reductive amination to produce primary amine compounds. The catalyst is prepared through the steps of: 1) preparing a MOF material ZIF-67; and 2) under protection of nitrogen gas, calcining the MOF material ZIF-67 at 200-1000 DEG C for 1-10 h to produce the nitrogen-doped carbon material supporting cobalt catalyst Co / N-C. The method of catalytic hydrogenation reductive amination to produce the primary amine compounds with the catalyst includes the steps of: in an organic solvent, adding a carbonyl compound, ammonia water and the nitrogen-doped carbon material supporting cobalt catalyst, feeding hydrogen gas, and performing a reaction at 50-150 DEG C under 0.1-5 MPa for 0.5-20.0 h to produce the amine compounds. The preparation method of the catalyst is simple in operations. The catalyst can be used for producing the primary amine compounds in a manner of catalytic hydrogenation reductive amination. In the method, the primary amine compounds are produced with the carbonyl compound as a raw material through catalytic hydrogenation by means of the catalyst, so that the method has mild reaction conditions and is high in yield.
Owner:SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES

Bifunctional polyethylene glycol and adriamycin conjugate and preparation method thereof

The invention relates to a bifunctional polyethylene glycol and adriamycin conjugate and a preparation method thereof. The bifunctional polyethylene glycol and adriamycin conjugate is prepared in the following steps: modifying methoxy polyethylene glycol which serves as a raw material through hydroformylation, carrying out a reductive amination reaction on the modified methoxy polyethylene glycol and disulfide-bond containing dihydrazide to generate terminal-hydrazide polyethylene glycol, and carrying out a reaction on the terminal hydrazide of the terminal-hydrazide polyethylene glycol and the ketone carbonyl of the adriamycin to generate a hydrazone bond to obtain the bifunctional polyethylene glycol and adriamycin conjugate. The bifunctional polyethylene glycol and adriamycin conjugate provided by the invention can adapt to the reductive acidic environment in a cancer cell to release drugs rapidly to improve the cancer treatment effect and reduce the drug resisting possibility of the cancer cell, and in addition, the bifunctional polyethylene glycol and adriamycin conjugate can be self-assembled into a nano particle in a water phase to be able to circulate for a long time in blood to improve the pharmacokinetics of the doxorubicin. The method for preparing the bifunctional polyethylene glycol and adriamycin conjugate has the advantages of simple process, mild reaction conditions, high drug carrying rate and low cost, and the raw materials are easy to obtain. The bifunctional polyethylene glycol and adriamycin conjugate has potential application values in the aspects of targeted delivery of drugs, controlled release of drugs and improvement of clinical cancer resisting and treating effects.
Owner:XI AN JIAOTONG UNIV

Benzothiazole-aniline compound used as pH fluorescent probe and preparation method thereof

The invention discloses a benzothiazole-aniline compound used as a pH fluorescent probe and a preparation method thereof. The structural formula is shown as a chemical formula (shown in the description) (I), wherein in the formula, R1 is vinyl, acetenyl, styryl, phenylethynyl, biphenyl or perylene base; and R2 and R3 are both hydrogen, methyl or ethyl alkane. The preparation method comprises the following steps of: taking p-bromobenzaldehyde and 2-aminothiophenol as raw materials, and connecting with iodine-containing nitrobenzene derivative through dehydration cyclization reaction and coupling reaction; and generating the pH fluorescent probe benzothiazole-aniline derivative through reductive amination. Rigid structures, such as benzothiazole and phenylethynyl, are introduced into the fluorescent probe; the fluorescent probe is high in fluorescence quantum efficiency, and high in thermal stability and solubility. The probe can detect pH value under strong acid condition by adopting a photoinduced charge transfer mechanism and a conjugate passivation mechanism; and the probe has the characteristics of rapid response, high sensitivity and high selectivity, and has wide application prospect in environment monitoring, ecological protection, disease diagnosis, industrial production and sewage inspection.
Owner:浙江富昇科技有限公司

Method for selective enrichment and identification of N-linked glycopeptide

The invention relates to a method for selective enrichment and identification of N-glycosylation sites in a biological sample based on a reductive amination reaction of amino and aldehyde groups and application of the method to proteomic analysis of N-glycoprotein. The method comprises the following steps: taking a biological sample containing glycoprotein, carrying out enzymatic hydrolysis by using trypsin and then blocking the terminated amino group and side-chain amino group of a peptide fragment by using formaldehyde; then oxidizing a sugar chain on glycopeptide by using a sodium periodate solution so as to produce an aldehyde group; then enriching oxidized glycopeptide with amino microspheres and carrying out treatment with peptide glycosidase PNGase F; and carrying out mass spectrometry on released N-glycopeptide so as to obtain proteome information of N-glycoprotein in the sample. The method can be used for proteomic analysis of glycosylation and can acquire identification results of corresponding glycoprotein, glycopeptide and glycosylation sites at the same time. The method is simple and highly efficient and has high throughput in identification of N-glycosylation sites on glycoprotein.
Owner:DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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