454426-80-3Relevant academic research and scientific papers
Synthetic method of vardenafil hydrochloride impurities
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Paragraph 0034; 0047; 0055; 0063; 0071; 0079, (2018/04/01)
The invention discloses a synthetic method of vardenafil hydrochloride impurities, which relates to the technical field of pharmaceutical and chemical industry. The synthetic method comprises the following steps: taking alanine (A) as a raw material to react with acetic anhydride, generating 2-acetaminopropionic acid (B), enabling the 2-acetaminopropionic acid (B) to react with ethyl oxalyl monochloride, and generating a reaction product (C); enabling 2-ethoxybenzamidine hydrochloride (D) to react with hydrazine hydrate, generating a reaction product (E), enabling the reaction product (E) to react with the reaction product (C), and generating an impurity intermediate I (F); and enabling the impurity intermediate I (F) to generate an impurity intermediate II (G) under the effect of phosphorus oxychloride; performing sulfonation reaction on the impurity intermediate II (G) to generate a reaction product (H); and dropwise adding N-ethylpiperazine into the reaction product (H) to obtain a target product (I) 4-ethoxy-3-(3,4-dihydro-5-methyl-4-oxo-7-propylimidazole[5,1-f][1,2,4]-trizone-ketone) benzenesulfonic acid. The method is low in production cost, low in requirement on reaction conditions, favorable for the industrialized production and higher in purity of target products.
IMIDAZO-, PYRAZOLOPYRAZINES AND IMIDAZOTRIAZINES AND THEIR USE
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Page/Page column 16, (2011/04/14)
The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological di
SUBSTITUTED IMIDAZOTRIAZINES
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Page/Page column 45-46, (2010/02/06)
The invention relates to novel substituted imidazotriazines, to methods for the production thereof, and to their use for producing medicaments for the treatment and/or prophylaxis of cancer and neurodegenerative diseases, particularly Parkinson's disease and schizophrenia.
HETERO-CYCLICALY SUBSTITUTED IMIDAZOTRIAZINES
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Page/Page column 42, (2010/02/06)
The invention relates to novel hetero-cyclically substituted imidazotriazines and a method for the production and use thereof for producing drugs which are used for curing and/or preventing cancers and neurodegenerative diseases, in particular Parkinson d
Substituted imidazotriazinones
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, (2008/06/13)
The present invention relates to new substituted imidazotriazinones, processes for their preparation, and their use for the production of medicaments, in particular for improving perception, concentration power, learning power and/or memory power.
2-Phenyl-substituited Imidazotriazinones as Phoshodiesterase Inhibitors
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Page 41, (2010/02/05)
2-(Sulfamoyl-substituted phenyl)-3H-imidazo (5,1-f) (1,2,4) triazin-4-ones (I) are new. Imidazotriazinones of formula (I) and their salts, N-oxides and isomeric forms are new: R1 = H or 1-4C alkyl; R2 = 1-4C straight chain alkyl; R3, R4 = H, 2-8C alkenyl, 1-8C alkoxy or 1-10C alkyl (optionally interrupted by O and/or substituted by a very wide range of specific groups); or R3 or R4 = NR20R21, adamantyl, 2,2-dimethyl-4-phenyl-1,3-dioxan-5-yl, sulfolanyl, hydroxy-sulfolanyl, 2-oxo-tetrahydrofuran-3-yl; or 3-8C cycloalkyl, 6-10C aryl or 5-7 membered heterocycle, all optionally substituted by specific groups; or NR3R4 = (a) optionally benzo-fused, saturated, partially unsaturated or unsaturated 5-7 membered heterocycle, optionally containing 1-3 of S, N, O and NR37 and optionally substituted by a very wide range of specific groups; or (b) a group of formula (i)-(iv); R20,R21 = H or 1-6C alkyl; R37 = H, OH, CHO, CF3, up to 4C acyl, up to 4C alkoxycarbonyl, 1-4C alkoxy, 1-6C alkyl (optionally substituted by specific groups) or -(CO)iE; i = 0 or 1; E = 3-7C cycloalkyl or benzyl; 6-10C aryl or 5- or 6-membered heteroaryl, both optionally substituted by specific groups ; or 5-methyl-1-oxo-2,1,3-oxadiazol-4-yl, N-methylpiperazino or morpholino; R5,R6 = H, 1-6C alkyl, OH or 1-6C alkoxy. The full definitions are given in the DEFINITIONS (Full Definitions) field. An Independent claim is included for the preparation of (I).
