- PROCESS FOR THE PREPARATION OF PRODUCING PYRAZOLO[1,5-A] PYRIMIDINE DERIVATIVES
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Processes and intermediates useful for producing pyrazolo[1,5-a] pyrimidine derivatives.
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Paragraph 0096
(2021/06/04)
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- Benzoaza-polycyclic compound and synthesis method thereof
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The invention discloses a benzoaza-polycyclic compound and a synthesis method thereof. The compound is prepared by taking beta-keto ester as an initial raw material, carrying out substitution and Wittig reaction on the raw material and (2-(bromomethyl)benzyl)triphenylphosphonium bromide under an alkaline condition, carrying out one-pot reaction to obtain a double bond-containing benzoaza-polycyclic ring, and then carrying out catalytic hydrogenation reduction. According to the invention, various benzoaza-polycyclic rings are synthesized by the one-pot method, the operation is simple and convenient, rapid preparation in a laboratory can be realized, and the prepared compound can be used as an important intermediate in the industries of medicines and pesticides.
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- With the biological activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compound and its preparation method and application (by machine translation)
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The invention discloses a has biological activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compound and its preparation method and application, which belongs to the with anti-tumor activity to the technical field of the synthesis of the compounds. The technical scheme of the present invention is to point: has biological activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compound, has the following structure:, wherein R1 For the ethyl carboxylic acid ester, ethylamine methyl, formyl methyl amine, dimethyl amino formyl, pyridine - 3 - methylene amino formyl, piperidine a acyl or anilino formyl, R2 For hydrogen or phenmethyl. The invention also discloses the has biological activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compound of preparation method and the preparation of anti-mammary tumor application of the medicament. The process of preparing the process is simple, easy to control, the target product high yield and good repeatability, prepared with anti-tumor activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compounds are all on breast cancer cell MCF - 7 has definite inhibitory effect. (by machine translation)
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- New P2X3 receptor antagonists. Part 2: Identification and SAR of quinazolinones
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Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clinical trials with the most advanced compound. We have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonistic properties. This Letter describes the SAR of a back-up series containing a 4-oxo-quinazoline central ring. The discovery of the highly potent compounds 51 is presented.
- Szántó, Gábor,Makó, Attila,Vágó, István,Hergert, Tamás,Bata, Imre,Farkas, Bence,Kolok, Sándor,Vastag, Mónika
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p. 3905 - 3912
(2016/08/01)
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- ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
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- Preparation method for 1-benzyl-3-piperidone hydrochloride
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The invention discloses a preparation method for N-benzyl glycine ethyl ester. The method comprises the following steps: dissolving benzylamine in an organic solvent I, then adding 2-halogenated ethyl acetate, alkali and quaternary ammonium salt, and performing reaction to obtain the N-benzyl glycine ethyl ester. The invention also discloses a preparation method for 1-benzyl-3-piperidone hydrochloride. The method comprises the following specific steps: (1) preparing an intermediate IV (N-benzyl glycine ethyl ester); (2) dissolving the intermediate IV in an organic solvent II, then adding 4-halogenated ethyl acetate and alkali, and performing reaction to obtain an intermediate III; (3) performing reaction between the intermediate III and the alkali, reversely regulating a pH value to 6-8, performing concentration under reduced pressure, extracting by using ethyl acetate, performing washing and drying, and then performing concentration under reduced pressure to obtain an intermediate II; (4) performing reaction on the intermediate II and acid, performing rotary evaporation concentration, and adding a crystal solvent for crystallization to obtain a product. The route synthesis steps are short, the process is novel, the intermediates are high in purity, the product yield is high, and the cost is low.
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- ANTI-ANGIOGENESIS COMPOUND, INTERMEDIATE AND USE THEREOF
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Disclosed are an anti-abnormal proliferation of angiogenesis compound represented by formula I, use and intermediate thereof. The compound has good effect against abnormal proliferation of angiogenesis, and the activity of the compound is produced by inhibiting VEGFR2. The compound can be used for treating diseases, such as wet macular degeneration, inflammation, malignant tumor and the like, caused by abnormity of angiogenesis and protein kinases such as VEGFR2, FGFR2 and the like.
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- PHENYL-HETEROARYL DERIVATIVES AND METHODS OF USE THEREOF
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The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.
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Page/Page column 88-89
(2011/09/19)
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- SULFONAMIDES AND PHARMACEUTICAL COMPOSITIONS THEREOF
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The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I).
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Page/Page column 74-75
(2008/12/04)
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- Process development and scale-up of a selective α1- adrenoceptor antagonist
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A synthetic route to a potent and selective α-1-adrenergic receptor antagonist has been developed and demonstrated in a pilot plant. The route has been used in two pilot plant campaigns and has produced RO3203546 in 2.3 and 12.0 kg batch sizes. The first pilot plant campaign focused primarily on the end-game of the process with particular emphasis on the development of a method to isolate the active pharmaceutical ingredient (API). The second pilot plant campaign allowed front-end process improvements to be demonstrated. The reiterative process improvements resulted in an economical process with improved throughput and product quality when compared to the original discovery synthesis.
- Connolly, Terrence J.,Matchett, Michael,Sarma, Keshab
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- ANTIPARASITIC TERPENE ALKALOIDS
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The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid compound of this invention as an effective ingredient in an antiparasitic formulation. More particularly, the present invention relates to derivatives of the terpene alkaloid (1S,2R,4aS,5R,8R,8aR)-2-(acetyloxy)-8a-hydroxy-3,8-dimethyl-5-(1-methylethenyl)-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl (2S,3aR,9bR)-6-chloro-9b-hydroxy-5-methyl-1,2,3,3a,5,9b-hexahydropyrrolo[2,3-c][2,1]benzoxazine-2-carboxylate. Pharmaceutical compositions comprising the same are also disclosed.
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- Anti-anoxic furo- or pyrrolo-pyridine compounds and pharmaceutical compositions containing them
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Pyridine derivatives of the general formula (I) STR1 in which X is --O-- or --NH--, R1 is a phenyl group optionally substituted by one or two halogen atoms or a methyl, ethyl, trifluoromethyl, methoxy or phenyl group or, when R2 is not a benzyl group, an amino group, or is a naphthyl or benzodioxanyl group, and R2 is hydrogen or a benzyl group, or when X is --O--, R2 can also be a methyl or ethyl group, and their pharmaceutically acceptable acid addition salts are useful as antianoxics.
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