139756-01-7Relevant articles and documents
A new process for the synthesis of sildenafil intermediate and resulting sildenafil intermediates (by machine translation)
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Paragraph 0044; 0052-0058, (2019/06/07)
The present invention discloses a new process for the synthesis of sildenafil intermediate and resulting sildenafil intermediate, which belongs to the technical field of pharmaceutical intermediates. The invention comprises the following steps: S1: nitration reaction to 1 - methyl - 3 - propyl pyrazole - 5 - carboxylic acid ethyl ester as the starting material, adopts concentrated sulfuric acid and concentrated nitric acid to the starting material to nitration, shall nitration product; S2: amidation reaction uses ammonium chloride and trimethyl aluminum of the nitration reagent to the aminolysis product aminolysis, quenching, separation, drying, evaporation of the solvent, shall be sildenafil intermediate 1 - methyl - 3 - propyl - 4 - nitryl pyrazole - 5 - carboxamide. The invention from an initial raw material to the target product only needing two-step reaction can be completed, the process flow is short, mild condition, a substantial increase in product yield, save a large number of strong acid, strong alkali and thionyl chloride and other inorganic irritation raw materials, will not cause corrosion of the apparatus, to reduce the large amount of waste water and waste acid, reduce the environmental pressure. (by machine translation)
NOVEL COMPOUNDS FOR USE IN COGNITION IMPROVEMENT
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, (2016/04/19)
Novel compounds for use in cognition improvement It relates to certain compounds having a polycyclic structure and a -(C=O)NRaRb moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases.
PYRAZOLOPYRIMIDINONES FOR THE TREATMENT OF IMPOTENCE AND PROCESS FOR THE PREPARATION THEREOF
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Page/Page column 47, (2015/09/23)
The present invention relates to Pyrazolopyrimidinone compounds as PDE5 inhibitors with better IC50 value, good in vivo efficacy and PK profile and a process for the preparation thereof. The present invention covers the pyrazolo pyrimidinone based compounds that have been designed, synthesized and screened for PDE5 inhibitory activity and its PDE5 inhibitory potential is provided in this invention. These designer compounds have shown nanomolar potency when screened for PDE5 inhibitory activity and also shown better in vivo efficacy. These compounds can be used in the treatment of male erectile dysfunction or in the treatment of impotence.