616224-61-4Relevant articles and documents
Synthetic method for Laquinimod intermediate 2-amino-6-chlorobenzoic acid
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Paragraph 0022; 0029; 0032; 0038; 0041; 0047; 0050, (2019/10/01)
The invention discloses a synthetic method for a Laquinimod intermediate 2-amino-6-chlorobenzoic acid. The synthetic method is characterized in that the 2-amino-6-chlorobenzoic acid can be obtained through the reaction of 3-chloro-2-methylaniline under the action of a protective agent and an oxidizing agent; and a reaction process includes the following steps: 1) uniformly mixing the 3-chloro-2-methylaniline, the protective agent and a solvent S1, performing stirring reaction for 1-2 h under 40-50 DEG C, and obtaining a mixture I at the end; 2) uniformly mixing the oxidizing agent, water and asolvent S2, introducing a protection gas, controlling a reaction temperature to be 145-155 DEG C and reaction pressure to be 5-7 atmospheric pressure so that a mixture II can be obtained, dropping the mixture I into the mixture II, controlling dropping time to be 50-70 min, then controlling the temperature to be 160-175 DEG C and the reaction pressure to be 8-10 atmospheric pressure, performing continuous reaction for 6-8 h, and obtaining a mixture III after cooling; 3) adding hydrochloric acid and a solvent S3 into the mixture III, controlling the reaction temperature to be 75-90 DEG C and the reaction pressure to be normal pressure, performing reaction for 0.5-1 h, and obtaining a mixture IV after cooling; and 4) adding a solvent S4 into the mixture IV, performing standing and layering,and concentrating, steaming and removing the solvents to obtain a product after an organic phase is washed by water and dried by a drying agent. The method is low in raw material cost and high in yield.
A phosgene and peroxide-free one-pot tandem synthesis of isatoic anhydrides involving anthranilic acid, boc anhydride and 2-chloro-N-methyl pyridinium iodide
Verma, Chhaya,Sharma, Somesh,Pathak, Arunendra
supporting information, p. 6897 - 6899 (2019/04/10)
A phosgene and peroxide-free approach for the synthesis of isatoic anhydrides has been described. The synthesis involves the carbamate formation with boc anhydride followed by in situ cyclization to afford the isatoic anhydride. The importance of this synthetic strategy is in the ease of operation, scalability and preparation from readily available raw materials.
PIPERIDINE DERIVATIVES HAVING CCR3 ANTAGONISM
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Page 456, (2008/06/13)
The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides compounds represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C1-C6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.
Sulfonamides having antiangiogenic and anticancer activity
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Page 53, (2008/06/13)
Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
Sulfonamides having antiangiogenic and anticancer activity
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, (2008/06/13)
Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
