- A method for preparing [...]
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The invention discloses a preparation method of indiplon. The preparation method of indiplon is characterized in that 2-acetyl thiophene is taken as a starting material, a DMFDMA condensation reaction is carried out under the action of an alkaline quaternary ammonium salt catalyst shown in a formula (II), a cyclization reaction is sequentially respectively carried out on the alkaline quaternary ammonium salt catalyst as well as hydroxylamine and aminoguanidine nitrate, and finally N-[3-[3-(dimethylamino)-1-oxyl-2-propenyl]-pheyl]-N-methyl acetamide is added for carrying out reaction, so that the target compound shown in a formula (I) is obtained, and the formula (I) and the formula (II) are described in the specification, wherein R is CC1-C10 N,N-dimethyl substituted alkyl. Compared with the prior art, the alkaline quaternary ammonium salt catalyst is used in a reaction process, and series reaction is carried out on multiple components, so that the preparation method of indiplon has the advantages of simple technological operation, good technical performance and no environment pollution.
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Paragraph 0034-0035
(2017/03/08)
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- Processes for the Preparation of Indiplon and Intermediates Thereof
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The present invention relates to processes for the preparation of indiplon and its polymorphic mixtures.
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- Salts And Co-Crystals of Pyrazolopyrimidine Compounds, Compositions Thereof And Methods For Their Production And Use
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The invention provides pharmaceutically acceptable salts and co-crystals of pyrazolopyrimidine compounds such as zaleplon, indiplon and ocinaplon, processes for their preparation, compositions comprising such salts and co-crystals and methods of using such salts and co-crystals for treating various diseases and conditions.
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Page/Page column 11
(2010/11/30)
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- Method of using substituted pyrazolo [1,5-a] pyrimidines
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This invention relates to novel methods of use of certain pyrazolo[1,5-a]pyrimidine compounds and the therapeutically acceptable salts thereof. This invention also relates to novel methods of using these compounds as anti-proliferative agents in mammals, including humans.
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Page/Page column 47
(2010/10/20)
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- HYDRATE OF N-METHYL-N-(3-{3-[2-THIENYLCARBONYL]-PYRAZOL-[1,5-α]- PYRAMIDIN-7-YL}PHENYL)ACETAMIDE AND PROCESSES AND METHODS RELATED THERETO
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A novel hydrate form of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide ("Compound No. 1") and processes related to the use thereof in the synthesis of a polymorphic form of Compound No. 1.
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Page/Page column 12
(2008/06/13)
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- TWO-PHASE METHOD FOR THE SYNTHESIS OF SELECTED PYRAZOLOPYRIMIDINES
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An improved method of making a substituted pyrazolopyrimidine. The method comprises reacting a aminopyrazole compound or a salt thereof with a substituted 1-oxo-2-propenyl-arene(-heterocycle) or a salt thereof under acidic conditions in a reaction medium including a two-phase mixture of an aqueous solution and a water-immiscible organic liquid. Specific substituted pyrazolopyrimidines include N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide and N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazolo[1, 5-a]-pyrimidin-7-yl}phenyl)acetamide.
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Page/Page column 12
(2008/06/13)
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- N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1, 5-α]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto
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N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide, and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Compositions containing N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide, as well as pharmaceutically acceptable salts thereof, are also disclosed.
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- Polymorphs of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto
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Polymorphs of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (Compound 1), and use of the same as a sedative-hypnotic, anxiolytic, anticonvulsant, and skeletal muscle relaxant agent. Processes for making the same, as well as related compositions and methods are also disclosed, particularly with regard to treatment of insomnia. A polymorph Form I possessing exception physical and heat stability is provided. A polymorph Form II
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