- Synthesis process of 2-amino-3-bromo-6-chloropyrazine
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The invention relates to a synthesis process of 2-amino-3-bromo-6-chloropyrazine, which comprises the following steps: 1) adding 2-amino-6-chloropyrazine into an organic solvent, cooling the system, and then adding a catalyst; (2) dropwise adding a bromination reagent, namely liquid bromine, into the system, after dropwise adding is finished, carrying out heat preservation reaction, and carrying out TLC detection and tracking reaction; and 3) adding a sodium sulfite solution into the system until reddish brown fades, extracting with chloroform, washing with water, drying with anhydrous sodium sulfate, concentrating, passing through a silicagel column roughly, and recrystallizing to obtain the yellow solid compound 2-amino-3-bromine- 6-chloropyrazine. 2-amino-3-bromine- 6-chloropyrazine is used as an initial raw material and is brominated to obtain the product, so that the method is simple to operate, short in step, easily available in raw material, simple to purify, high in yield, low in cost and easy for large-scale production.
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Paragraph 0022-0030
(2021/05/01)
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- MANUFACTURE OF COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2
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The present invention relates to a method for the manufacture of a compound of Formula I or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme: wherein LG, A, n, m and p are as defined in the Summary of the Invention.
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Paragraph 00237; 00240
(2020/05/12)
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- PROCESS OF MANUFACTURE OF A COMPOUND FOR INHIBITING THE ACTIVITY OF SHP2
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The invention relates to a method for the manufacture of a compound of Formula I as mentioned above, or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II wit
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Paragraph 00308; 00312
(2020/05/12)
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- Large-scale process for preparing 2-amino-3-bromo-6-chloropyrazine
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The invention discloses a large-scale process for preparing 2-amino-3-bromo-6-chloropyrazine. The product is obtained from 3-aminopyrazine-2-carboxylate as a raw material through steps of chlorination, diazotization bromination, ester group hydrolysis, carboxyl rearrangement, t-butyloxycarbonyl removal and the like. The process is higher in yield, simple in purification, prone to large-scale production and capable of realizing effective and low-cost production.
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Paragraph 0031; 0044-0046
(2018/06/26)
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- COMPOUNDS FOR USE IN ANTIBACTERIAL APPLICATIONS
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The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods or uses as antibacterials for bacterial infections.
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Page/Page column 67; 68; 126; 127
(2017/03/14)
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- SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS
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The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These co
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Page/Page column 104
(2016/12/07)
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- TRICYCLIC DLK INHIBITORS AND USES THEREOF
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The invention relates to compounds of formula (I) and salts thereof, wherein ring A and R1-R2 have any of the values defined in the specification. The compounds and salts are useful for treating DLK mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as methods of using said compounds, salts, or compositions as DLK inhibitors and for treating neurodegeneration diseases and disorders.
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Page/Page column 78
(2016/09/26)
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- ANTICANCER PYRIDOPYRAZINES VIA THE INHIBITION OF FGFR KINASES
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The invention relates to new pyridopyrazine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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Page/Page column 133; 134
(2013/05/21)
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- INHIBITORS OF JAK
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The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
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Page/Page column 88-89
(2011/04/18)
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- BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
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Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Page/Page column 88-89
(2011/06/16)
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- PYRAZOLE COMPOUNDS
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The present invention is directed to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
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Page/Page column 79
(2009/03/07)
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- Pyrazine compounds
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A compound of formula (I) wherein R1is selected from the group consisting of phenyl substituted by one or more halogen atoms, naphthyl and naphthyl substituted by one or more halogen atoms; R2is selected from the group consisting of —NH2and —NHC(═O)Ra; R3is selected from the group consisting of —NRbRc, —NHC(═O)Raand hydrogen, R4is selected from the group consisting of hydrogen, -C1-4alkyl, -C1-4alkyl substituted by one or more halogen atoms, —CN, —CH2OH, —CH2ORdand —CH2S(O)xRd; wherein Rarepresents C1-4alkyl or C3-7cycloalkyl, and Rband Rc, which may be the same or different, are selected from hydrogen and C1-4alkyl, or together with the nitrogen atom to which they are attached, form a6-membered nitrogen containing heterocycle, which heterocycle can be further susbtituted with one or more C1-4alkyl; Rdis selected from C1-4alkyl or C1-4alkyl substituted by one or more halogen atoms; x is an integer zero, one or two; and pharmaceutically acceptable derivatives thereof; with the proviso that R1does not represent (a); when R2is —NH2, and both R3and R4are hydrogen.
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