117 results about "Pyrimidifen" patented technology

The invention relates to pyrimidinamine and pyridinamine Hedgehog signal conduction inhibitors. The inhibitors are compounds with the structure represented by formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to a medicinal use of the above compounds as hedgehog signal conduction inhibitors.

The invention discloses preparation methods and biological activity of amino acid ester type compounds containing 4-(dimethoxymethyl)pyrimidine heterocycle for prevention and treatment of tobacco mosaic viruses, namely compounds as shown in the following general formula (I) and preparation methods thereof. The invention introduces amino acid ester type compounds containing 4-(dimethoxymethyl)pyrimidine heterocycle synthesized by a one-pot process under an ultrasonic condition by taking 4-(dimethoxymethyl)pyrimidine-2-amine, substituted aldehyde and malonic ester as raw materials and takes toluene as a solvent. The compounds I5 and I8 disclosed by the invention have better inhibition effects on tobacco mosaic viruses and ralstonia solanacearum. The compounds are shown in the description.

The invention relates to an acaricide composition prepared by using pyrimidifen and etoxazole as main ingredients and adding emulsifier as well as organic solvent. The composition has the advantages of special effects on preventing and eliminating mite and ovum thereof, larva and nymphae, simple processing technique, no three wastes and convenient use.

The present invention relates to a compound containing 4-bromo-2-(4-chlorophenyl)-1-ethoxymethyl-5-( trifluomethyl) pyrrol-3-formonitrile and one or several kinds selected from pyrazole, imidazole, triazole, pyrimidine amine and thiocarbamate, etc. Said invention can effectively be used for preventing and controlling the injurious insects, mites and diseases of cotton, fruit tree, tea, vegetable,flower and crops, etc.

The present invention relates to new organic compound, and is especially the preparation process of N-(2-methyl-5-nitro) phenyl-4-(3-pyridyl) pyrimidiyl-2-amine as the key intermediate for imatinib, which is tyrosine protein kinase inhibitor for treating chronic myeloid leukemia and other diseases, and its analog N- phenyl-pyrimidiyl-2-amine derivative. The target product may be prepared through condensation of 4-aromatic heterocycle-2-halogenated pyrimidine and substituted aniline in the presence of catalyst. The preparation process has low material cost, scientific synthesis path, high product yield and other advantages.

The invention discloses an N-[(3R,4R)-1-benzyl-4-methylpiperidine-3-yl]-N-methyl-7H-pyrrolo[2,3-d] pyrimidine-4-amine crystal and a preparation method thereof. The method comprises steps as follows: firstly, 4-chloro-7-(p-tolylsulfonyl) pyrrolo [2,3-d] pyrimidine, 1-benzyl-4-methyl-3-aminomethyl dihydrochloride, potassium carbonate and water are added to a reaction vessel sequentially, heated and subjected to thermal insulation, and white solids are obtained; the white solids, sodium hydroxide and n-butyl alcohol are added to the reaction vessel sequentially, an obtained organic phase is washed with water, then anhydrous magnesium sulfate is added to the organic phase for dehydration, and a dichloromethane extracting solution is obtained; finally, eluting and curing are performed, and the crystal is obtained. The purity of the crystal is higher than 99.9%. According to a final product tofacitinib citrate synthesized with the intermediate, related substances are controlled to be lower than 0.1%, and the preparation of the crystal has great technical advantage and research value.

The invention provides a deuterated benzimidazole-pyrilamine derivative which is a compound shown in formula (I) shown in the specification or a pharmaceutically acceptable salt, a monocrystal substance or a polymorphic substance of the compound as well as an application of the derivative to preparation of drugs for treating cancer, and further provides pharmaceutical composition containing the compound. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 refer to hydrogen or deuterium independently, and at least one deuterium is contained in total. The deuterated benzimidazole-pyrilamine derivative mesylate prolongs half-life periods of the drugs, prolongs the retention time of the drugs in human bodies and increases concentration of the drugs in blood, so that the better curative effect can be realized.

The present invention relates to a novel N-phenyl-2-pyrimidine-amine derivative represented by the above formula (1) and its salt showing a superior effect on cancer in warm-blooded animals, such as lung cancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer, breast cancer, chronic or acute leukemia, hematologic malignancy, encephalophyma, bladder cancer, rectal cancer, cervical cancer, lymphoma, etc. The present invention also relates to a process for preparing the compound, and to a pharmaceutical composition for the treatment of the above various diseases, which comprises an effective amount of the compound as an active ingredient together with pharmaceutically acceptable inert carriers.

A synergistic composite insecticide for preventing and treating cabbage caterpillar and rice borer contains two primary active components including high-effect cyfluthrin, assistant and excipient.

The invention relates to a synthesis method of imatinib and imatinib mesylate. The method comprises the following steps: condensing 3-acetylpyridine and N,N-dimethylformamide dimethyl acetal which aretaken as initial raw materials to obtain 3-dimethylamino-1-(3-pyridyl)-2-propen-1-one, then reacting with 2-methyl-5-nitrophenylguanidine nitrate to form a pyrimidine ring, performing nitro reductionto obtain N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine, amidating the N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine and 4-(chloromethyl)benzoyl chloride, performing affinitysubstitution with 1-methylpiperazine to obtain imatinib, and salifying the imatinib and methanesulfonic acid. The products obtained by the method have the advantages of few impurities, simplicity in post-treatment, high total yield, greenness, environmental protection and safety, and is suitable for a production process for large-scale industrial production of imatinib mesylate.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a tofacitinib citrate intermediate as well as a preparation method and an application thereof. Whereinthe tofacitinib citrate intermediate is N-methyl-N-((3R, 4R)-4-methylpiperidine-3-yl)-7H-pyrrolo [2, 3-D] pyrimidine-4-amine dihydrochloride monohydrate. The preparation method comprises the followingsteps: adding N-methyl-N-((3R, 4R)-1-benzyl-4-methylpiperidine-3-yl)-N-methyl-7H-pyrrolo [2, 3-d] pyrimidine-4-amine into water and an organic solvent, then adding hydrochloric acid and palladium hydroxide carbon, introducing hydrogen to react, and filtering out the palladium hydroxide carbon; cooling to room temperature, dropwise adding an organic solvent, crystallizing, carrying out suction filtration, and drying to obtain the tofacitinib citrate intermediate. The method greatly improves the utilization rate of raw materials, reduces the production cost, and improves the product quality.

Preparation methods of N-(2-methylpyridyl-5-nitro-3)-4-(3-pyridinyl)pyrimidin-2-amine and an intermediate thereof are characterized in that N-(2-methylpyridyl-5-nitro-3-)-4-(3-pyridinyl)pyrimidin-2-amine is prepared through three step reactions by taking 2-sulfydryl-4-(3-pyridinyl)pyrimidine as a raw material; wherein 2-sulfydryl-4-(3-pyridinyl)pyrimidine is subjected to combination of two reactions comprising iodomethane methylation and oxidation by one-pot synthesis to direct synthesize 2-methylsulfonyl-4-(3-pyridinyl)pyrimidine; then the prepared compound 2-methylsulfonyl-4-(3-pyridinyl)pyrimidine by using the above method is reacted with a raw material compound 2-amino-4-nitrotoluene to obtain the product N-(2-methylpyridyl-5-nitro-3-)-4-(3-pyridinyl)pyrimidin-2-amine. The preparation methods have the advantages that no organic solvent is needed to add during the whole process, product processing is simple, yield is high and pollutant discharge is less.

Disclosed herein are tricyclic compounds, including pyrimido[4',5':4,5]thieno[2,3-c]pyridazine-8-amine, pyrido[3',2M,5]thieno[3,2-d]pyrimidine-4-amine, pyrazino[2',3':4,5]thieno[3,2-d]pyrimidin-4-amine, pyrido[3',2':4,5]furo[3,2-d]pyrimidin-4- amine, and pyrimido[4',5':4,5]furo[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholinereceptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disordersassociated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

The invention discloses a preparation method of N-((3R, 4R)-1-benzyl-4-methyl pyridine-3-yl)-N-methyl-7H-pyrrolo-[2, 3-d] pyrimidine-4-amine. The method takes sodium hydroxide as alkali and methyl alcohol as a solvent, and the intermediate N-((3R, 4R)-1-benzyl-4-methyl pyridine-3-yl)-N-methyl-7H-pyrrolo-[2, 3-d] pyrimidine-4-amine is obtained in a reaction of N-((3R, 4R)-1-benzyl-4-methyl pyridine-3-yl)-N-methyl-7-toluenesulfonyl-7H-pyrrolo-[2, 3-d] pyrimidine-4-amine. The method is high in yield, fewer in by-products and simple and convenient to operate, thus being both suitable for small-scale laboratory preparation and large-scale industrial production.

The invention discloses compounds represented by the formula (I), stereoisomers, pharmaceutically acceptable salts, or solvates thereof. The invention also provides an application of the abovementioned compounds in the preparation of antitumor drugs, angiogenesis inhibitors, EFGR kinase inhibitors, or AUR A kinase inhibitors.

The invention relates to a preparation method of imatine, and belongs to the technical field of medicine synthesis. In order to solve the problem of low product yield in the prior art, the invention provides the preparation method of the imatrine, which comprises the following steps: under the action of a catalytic amount of nitroreductase and coenzyme, converting a compound N-(2-methyl-5-nitrophenyl)-4-(3-pyridyl)-2-pyrimidinamine shown as a formula II into the imatrine through an enzymatic reaction; wherein the nitroreductase is as shown in SEQ NO1. According to the method, nitryl can be effectively and efficiently converted into amino, other by-products cannot be generated due to side reaction of the raw materials in the reaction process, the method has the advantages of being low in impurity content and high in product conversion rate, and the product yield reaches 97% or above.

The invention relates to a substituted benzo or pyridopyrimidine amine inhibitor as well as a preparation method and application thereof. Specifically, the compound has a structure as shown in a formula (I), the invention further discloses a preparation method of the compound and application of the compound as an SOS1 inhibitor, and the compound has a very good selective inhibition effect on SOS1 and has better pharmacodynamic and pharmacokinetic performance and lower toxic and side effects.

The invention relates to a mite-killing composition containing pyrimidifen and pyridaben. An active ingredient is formed by compounding pyrimidifen and pyridaben in a binary manner, wherein the mass ratio of the pyrimidifen to the pyridaben is (1-40):(40-1). The total mass of the active ingredients of the pyrimidifen and the pyridaben in a preparation accounts for 1%-80% of the mass of the whole preparation, and the balance is an auxiliary ingredient which is allowable and acceptable in pesticides. The mite-killing composition can be prepared into forms such as missible oil, suspending agent, wettable powder, water dispersible granules, emulsion in water and microemulsion. The mite-killing composition can be used for preventing tetranychid mites and rust mites on oranges, apples, pears, hawthorns, cottons, tobaccos, tea leaves, vegetables, ornamental plants and the like.

The invention provides a (substituted phenyl) (substituted pyrimidine) amido derivative as shown in a general formula (I) defined in the description, an optical isomer thereof, a pharmaceutically acceptable salt or eutectic, a preparation method thereof, and application thereof in preparation of tumor drugs. The general formula is a compound (I).

The invention relates to an application of composition containing a heterocyclic compound in preparation of a drug for treating leukemia. On one hand, the invention provides an application of composition containing pyridyl pyrilamine compounds in preparation of the drug for treating the leukemia; on the other hand, the invention provides an application of composition containing phenyl aminoformylthiazole compounds in preparation of the drug for treating the leukemia; and the invention provides an application of quinoline compounds in preparation of the drug for treating the leukemia.

Prostate cancer and hematological neoplasms are treated by administration of (i) a compound of Formula I: wherein: R¹ is —OH or —O—P(O)(OH)₂; and R² is (II) or (III); (ii) N⁶-benzyladenosine, (iii) N-(phenylmethyl)-7-β-D-ribofuranosyl-7H-pyrrolo [2,3 -d]pyrimidin-4-amine, (iv) N-(phenylmethyl)-7β-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine 5′-monophosphate; or a pharmaceutically acceptable salt thereof.

The application belongs to the field of medicinal chemistry, and relates to salts of substituted pyrrolopyrimidine CDK inhibitors, in particular to the compound 7-cyclopentyl-6-N, N-dimethylcarbamoyl-N-(5-(1,2 ,3,6-4H-pyridin-4-yl)pyridin-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine maleate (compound of formula II), compound of formula II The crystal form, its preparation method and pharmaceutical composition also relate to the use of the compound salt and its pharmaceutical composition in the preparation of medicines for treating diseases related to the inhibition of CDK4 and/or CDK6.