- A 5 - bromo -2 - methyl nicotinic acid ethyl ester
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The invention discloses a 5 - bromo - 2 - methyl nicotinic acid ethyl ester synthetic method, comprises the following steps: the acetyl ethyl acetate and alkali A adding solvent in the B enolizable; adding intermediate III and DABCO reaction; adding ammonium to cyclization; adding water quenching, organic solvent extraction C; removing the organic solvent to be crystalline crude product shall C; to be crystalline crude product recrystallized from 5 - bromo - 2 - methyl nicotinic acid ethyl ester; the invention to Meck development of 5 - chloro - 2 - methyl nicotinic acid ethyl ester is based on, through changing the reaction solvent and reduce the reaction temperature, significantly improves the stability of the intermediate III, so that the reaction can be smoothly to obtain the product, after treatment through recrystallization purification, thus avoiding the time-consuming column chromatography process, the average yield of 70%, the purity of 99.0% or more, is suitable for the large-scale industrial production.
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Paragraph 0053; 0054; 0055
(2019/02/13)
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- NOVEL 5 OR 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
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Disclosed herein are 5 or 8-substituted imidazo[l,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[l,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8- substituted imidazo[l,5-a]pyridines that can be useful for inhibiting indoleamine 2,3- dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.
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Paragraph 0444
(2016/10/31)
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- SUBSTITUTED METHYL ARYL OR HETEROARYL AMIDE COMPOUNDS
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This invention provides a compound of the formula (I), wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 in
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Page/Page column 59
(2008/06/13)
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- COMBINATIONS COMPRISING ALPHA-2-DELTA LIGANDS
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The instant invention relates to a combination of an EP4-receptor antagonist and an alpha-2-delta ligand, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly inflammatory,
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Page/Page column 208
(2008/06/13)
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