41 results about "Methyl-1H-indole" patented technology

The invention relates to a synthetic method of an anti-tumor medicine, namely N-[2-[[2-(dimethylamino) ethyl] methyl amino]-4-methoxy-5-[[4-(1-methyl-1H-indole-3-yl)-2-pyrimidyl] amino] phenyl]-2-acrylamide (AZD9291) and a key intermediate of the anti-tumor medicine. The synthetic method comprises the following steps: performing Boc acid anhydride protection on 4-fluoro-2-methoxy-5-nitroaniline to obtain 4-fluoro-2-methoxy-5-nitroanilino tert-butyl formate, then reacting with N,N,N'-trimethylethylenediamine to obtain 4-(N,N,N'-trimethylethylenediamino)-2-methoxy-5-nitroanilino tert-butyl formate, then reducing to obtain 2-(N,N,N'-trimethylethylenediamino)-4-methoxy-5-tert-butyl carbamate phenylamine, then completely reacting with acryloyl chloride and directly removing a Boc protecting group to obtain 2-methoxy-4-N,N,N'-trimethylethylenediamino-5-acrylamido phenylamine, and finally reacting with 3-(2-chloropyrimidine-4-yl)-1-methylindole to obtain AZD9291. A process disclosed by the invention is simple in step, relatively high in yield, mild in reaction condition and easy for realization of industrial production.

The invention discloses a preparation method for 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-indole as shown in the specification. The preparation method comprises the following steps: (1) subjecting a compound II and a compound III to a condensation reaction in an alcohol solvent under the action of alkali; and (2) mixing a reaction solution obtained in the step (1) with protonic acid and carrying out Bischler-Mohlau indole cyclization. Compared with the prior art, the invention has the following advantages: the condensation reaction in the first step and Bischler-Mohlau indole cyclization at the second step are integrated into a one-pot reaction, so operation is simple and convenient; a reaction product I is directly precipitated from the reaction solvent, so reaction post-treatment is substantially simplified, and high purity and high reaction yield are realized; and the method is applicable to enlarged production.

Provided in the present invention are a use of quinoline derivatives for treating oesophageal cancer and a treatment method, a pharmaceutical composition and a kit thereof. The 1-[[[4-(4-fluoro-2-methyl-1H-indole-5-yl)oxy-6-methoxyquinoline-7-yl]oxy]methyl]cyclopropylamine provided by the present invention can effectively treat oesophageal cancer, and reduce the sum of the diameters of patient's target lesions.

The invention discloses a method for synthesizing a natural product (+ / -)-folicanthine and an intermediate product thereof, belonging to the field of medicine. The method for synthesizing the intermediate product comprises the steps of: dissolving 4-methyl-N-(2-(1-methyl-1H-indole-3-)ethyl) p-toluenesulfonamide and Cs2CO3 in a solvent; adding a catalyst; and stirring to obtain the intermediate product. The method for synthesizing the natural product comprises the steps of: preparing the intermediate product; adding sodium in tetrahydrofuran to generate a sodium-naphthalene solution; adding the sodium-naphthalene solution into a tetrahydrofuran solution of the intermediate product to prepare a compound c; and adding sodium triacetoxyborohydride and formalin into an acetonitrile solution of the compound c, stirring, dropwise-adding an ammonia-saturated mixed solution of methanol and methylene dichloride, and concentrating and purifying a reactant to obtain the natural product. The method disclosed by the invention has the advantages of less reaction steps, environment friendliness in reaction, no use of metallic catalyst, high yield rate, moderate reaction conditions, no need of further treatment of the solvent and less pollution to the environment.

The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses.Novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, their esters of the general formula 1 and pharmaceutically acceptable salts and / or hydrates thereof have been disclosedwherein: R1 represents amino group substituent selected from hydrogen, optionally substituted C1-C5 alkyl, acyl or sulfonyl; R2 and R4 independently of each other represent alkyl substituent selected from hydrogen, halogen, optionally substituted C1-C3 alkyl, optionally substituted hydroxyl, optionally substituted amino group, optionally substituted aminomethyl, substituted mercapto group; R3 represents hydrogen, optionally substituted lower C1-C5 alkyl; R5 represents cyclic system substituent selected from hydrogen, fluorine, trifluoromethyl, carboxy group, alkyloxycarbonyl, possibly substituted aryl, heterocyclyl, optionally substituted aminomethyl, cyano group; R6 represents hydroxyl group substituent selected from hydrogen, optionally substituted C1-C5 alkyl, acyl.