87673-88-9Relevant academic research and scientific papers
Method for synthesizing methyl 1-methyl-imidazolyl-2-formate derivative
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Paragraph 0028-0030; 0037-0039, (2020/04/17)
The invention provides a method for synthesizing a methyl 1-methyl-imidazolyl-2-formate derivative, and particularly relates to the technical field of medicines. The method comprises the following steps: S1, taking 3-methylhistamine dihydrochloride shown in the formula (II) as an initial raw material, carrying out a cyclization reaction process on the raw material and formaldehyde, and carrying out aftertreatment to obtain a compound 1-methyl-4, 5, 6, 7-tetrahydro-1H-imidazo[4, 5-c]pyridine shown in the formula (III), S2, enabling the N-5 site of the compound shown in the formula (III) to react with di-tert-butyl dicarbonate to generate a compound tert-butyl 1-methyl-6, 7-dihydro-1H-imidazo[4, 5-C]pyridin-5-(4H)-carboxylate shown in the formula (IV), S3, making active hydrogen at the C-2 site of the compound (IV) react with butyl lithium to generate a lithium salt, and then making the lithium salt react with carbon dioxide to generate a compound tert-butyl 1-methyl-6, 7-dihydro-1H-imidazo[4, 5-C]pyridin-5-(4H)-carboxylate-2-carboxylic acid shown in the formula (V), and S4, carrying out a condensation reaction process on the compound shown in the formula (V) and methanol to obtain the target compound shown in the formula (I). The method has the advantages of cheap and accessible raw materials, high reaction yield and low production cost, and can easily implement industrialization.
PRMT5 INHIBITORS AND USES THEREOF
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, (2016/04/20)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof:wherein Y1 is of formula (?) or formula (y):Ring Y is a 5- to 6-membered heteroaryl ring; and V4, V5, Rx, x, y, and n are as defined herein. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
Anti-ulcer and antisecretory activity of selected imidazopiperidines
Arcari,Bernardi,Cimaschi,Falconi,Luini,Scarponi
, p. 1467 - 1471 (2007/10/02)
New thioureas and ureas with an interesting anti-ulcer and antisecretory activity are presented. The chemical synthesis, determination of the structure, and structure-activity relationships of the compounds are discussed.
