38results about How to "Pharmaceutically active" patented technology

The invention relates to the field of medicines, in particular to a lactam derivative and application thereof, and more specifically relates to a lactam derivative and a pharmaceutical composition containing the same as well as application of the composition and the lactam derivative to the preparation of a drug for prevention or treatment of nervous and mental diseases. The lactam derivative has a structure shown as a formula I.

The invention discloses an aspirin-based carbon quantum dot and application thereof in aspects of cell imaging and anti-inflammatory treatment, belonging to the technical field of nano-drugs. The invention in particular relates to a carbon quantum dot with strong fluorescent properties prepared from a hydrazine hydrate solution by utilizing a microwave heating method under the condition that aspirin dissolution is promoted. The carbon quantum dot prepared by the method is very stable under hyper-salt concentration and physiological pH conditions, blue-fluorescence is maintained, the carbon quantum dot can enter the cell nucleus, and the cells are effectively traced; and meanwhile, the original anti-inflammatory effect of aspirin is remained, and inflammatory cells can be effectively inhibited in an acute inflammation model constructed by utilizing carrageenin. In addition, the prepared aspirin carbon quantum dot is low in toxicity and does not influence liver and kidney functions and organs such as the heart, liver, spleen and kidney in in-vivo application, and the aim that the nanometer material has dual effects of diagnosis and treatment can be achieved.

The invention provides an omarigliptin intermediate preparation method. The omarigliptin intermediate preparation method comprises the step of mixing a compound I with a catalyzing enzyme, and reacting to obtain an omarigliptin intermediate. The omarigliptin intermediate preparation method has the beneficial effects that the cost of raw materials is reduced; the problem in the prior art that isomer byproducts are generated during preparation of the omarigliptin intermediate and cannot be utilized is effectively solved; the yield and atom economy are increased; and the omarigliptin intermediate preparation method is simple in operation, mild in conditions, environment-friendly and suitable for industrial production.

The invention relates to a trifluoroethanol/difluoroethanol reagent and a preparation method and an application thereof, the chemical structural formula of the trifluoroethanol reagent is shown in thespecification, in the formula, R1, R2 and R3 represent substituent groups on silicon atoms, and R1, R2 and R3 are independently selected from aryl, heteroaryl and alkyl respectively. The trifluoroethylation reagent and the difluoroethylation reagent provided by the invention can be used as synthesis intermediates of a plurality of organic compounds, some of the compounds have pharmaceutical activity, the preparation steps of the compounds are simplified, and the synthesis method is mild in condition and wide in substrate applicability.

The invention discloses a trifluoromethyl allyl compound as well as a preparation method and application thereof. According to the method, allyl alcohol is directly used as a raw material, CF3SO2Na is selected as a trifluoromethylation reagent, a metal-free and cheap photooxidation reduction catalyst is used, and under the catalysis of an organic photooxidation reduction agent, a byproduct SO2 generated in situ is reused as an activated C-OH bond, so that the reaction is carried out in an environment-friendly manner under a mild condition. The allyl alcohol used in the preparation method disclosed by the invention is a MoritA-Baylis-Hillman alcohol allyl alcohol raw material which is simple to synthesize and high in conversion rate, the applicable substrate range is wide, and the preparation cost is low. In addition, the preparation method disclosed by the invention is simple in steps, and has the characteristics of convenience in operation, environment friendliness, excellent stereoselectivity and broad-spectrum functional group tolerance. The trifluoromethyl allyl compound provided by the invention is a general precursor for preparing related CF3 molecules, has potential pharmaceutical activity and biological activity, and can be widely applied to biological and pharmaceutical active molecules.

The invention relates to a chiral aminoindoline derivative and a preparation method and application thereof.The chiral aminoindoline derivative has pharmaceutical activity or can be used for preparing a chiral aminoindoline derivative precursor with pharmaceutical activity, the preparation steps are simple, the conditions are mild, and the chiral aminoindoline derivative is suitable for industrial production. The technical problems that in the prior art, a chiral amino indoline derivative synthesis catalyst is expensive, and reaction conditions are harsh are solved.