9 results about "Drug synthesis" patented technology

This invention belongs to the field of pharmaceutical synthesis technology, specifically relating to a diarylurea derivative, its preparation method, and its application. The diarylurea derivative of this invention is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which exhibits high inhibitory activity against wild-type (WT), mutant G595R, and G667C tropomyosin receptor kinase (TRK), and can be used to treat NTRK fusion-positive locally advanced or metastatic solid tumors.

This invention belongs to the technical field of drug synthesis, specifically relating to memantine derivatives, their synthetic methods, and applications. The memantine derivatives include intermediate structural formulas I, II, and III, as well as a general structural formula. The linker is a substituted or unsubstituted C6-C10 aryl group, R1 is hydrogen or a C1-C6 alkyl group, and R2 is hydrogen, a C1-C6 alkyl group, or a nitrogen-containing or nitrogen-free structural fragment, or the overall structure of R1 and R2 is an N-substituted heterocyclopentyl or heterocyclohexyl group. The memantine derivatives provided by this invention improve drug activity by combining the memantine group with the OAB-14 partial structure, thereby altering the core structure. This invention also provides a synthetic method for the obtained compounds used in the treatment of Alzheimer's disease and Parkinson's disease.

This invention belongs to the field of pharmaceutical synthesis technology, specifically relating to indomethacin derivatives, their synthesis methods, and applications. The derivatives possess the chemical structures described in formulas (I), (II), and (III). This invention is the first to propose a series of novel indomethacin derivatives. Furthermore, this invention also proposes a synthesis method for indomethacin derivatives, using 5-hydroxy-1-indanone as a base material, to obtain the indomethacin derivatives of this invention through a series of reactions. This synthesis method yields high-yield products that are easily separated, making it the optimal method for preparing the indomethacin derivatives of this invention. Bioassays have confirmed that the indomethacin derivatives provided by this invention exhibit good toxic activity against aphids, spider mites, and armyworms, and can be applied to the control of plant pests.

The present application relates to the technical field of drug synthesis, and in particular to a synthesis method of racemic 2,6-dimethyl-2,3-dihydro-1H-inden-1-amine, which introduces amino through a conjugate addition reaction and a nucleophilic substitution reaction under the catalysis of cuprous iodide and other copper reagents by using N-acetyl-N-1-propenylacetamide and 2-fluoro-1,4-dimethylbenzene, and then hydrolyzes under alkaline conditions to obtain the racemic 2,6-dimethyl-2,3-dihydro-1H-inden-1-amine conveniently; the present application provides a more efficient, safe and economic solution for related synthesis reactions, has a wide application prospect, provides a new idea and method for the synthesis of such compounds, and improves the synthesis efficiency and quality of drugs.

The application provides a semi-florin chemotherapy drug and a synthesis method thereof, relates to the technical field of drug synthesis, and the semi-florin derivative exhibits significant selective anti-tumor activity, and the mechanism of action is that after entering tumor cells, the semi-florin derivative can induce the increase of the level of reactive oxygen species (ROS) in the cells, causes the collapse of the mitochondrial membrane potential, and finally triggers the late apoptosis pathway of the cells.

The application belongs to the technical field of medicine synthesis and application, and particularly relates to OAB derivatives, a synthesis method and application thereof. The OAB derivative has a structural formula, wherein R is,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, or. The synthesis method comprises the following steps: adding

The invention relates to the technical field of medicine synthesis, in particular to a synthesis method and application of a 2-(3, 4-dimethoxybenzamido) thiazole-4-amide derivative. The structure of the thiazole is as shown in a formula I in the specification. The preparation method of the 2-(3, 4-dimethoxybenzamido) thiazole-4-amide derivative comprises the following step: reacting a compound shown in a formula I with a compound shown in a formula II in the presence of HATU, DIPEA, primary amine or secondary amine and tetrahydrofuran to obtain the 2-(3, 4-dimethoxybenzamido) thiazole-4-amide derivative. The 2-(3, 4-dimethoxybenzoylamino) thiazole-4-amide derivative disclosed by the invention has a relatively good effect of relieving the Alzheimer's disease, and is characterized by having relatively strong cholinesterase inhibitory activity.

The application discloses a method for preparing chiral aryl-substituted alkenyl beta-hydroxy ester. The method constructs a biological catalysis reaction system in a phosphate buffer solution, and comprises a substrate shown in formula B, coenzyme NADP + , glucose, glucose dehydrogenase, and ketoreductase, and performs a stereoselective reduction reaction at 20-40 DEG C, so as to convert the substrate shown in formula B into chiral aryl-substituted alkenyl beta-hydroxy ester shown in formula A. The ketoreductase is selected from RasADH or RasADH-E189D. By using the method, green and efficient synthesis of chiral aryl-substituted alkenyl beta-hydroxy ester can be realized, and the method has important application value in the field of chiral drug synthesis.

The present application provides a novel double-stranded siRNA, conjugates thereof and uses thereof. The present application also provides uses of the double-stranded siRNA and conjugates thereof in the preparation of a medicament for treating and / or preventing hepatitis B disease. The present application relates to a novel compound, and uses of the compound in the raw material for DNA nucleotide solid-phase synthesis, the raw material for siRNA drug synthesis, the research of siRNA drug, the research of gene function and / or the screening of whole gene library, especially in the raw material for the synthesis of the double-stranded siRNA drug. Furthermore, the present application also relates to a novel nucleotide residue, and its application in the research of siRNA drug, the research of gene function and / or the screening of whole gene library, and its application as an oligonucleotide intercalating group.