- Synthesis method of 6-bromophthalazine
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The invention relates to a synthetic method of 6-bromophthalazine. The synthetic method comprises the following steps: 1) taking 4-bromo-1,2-xylene as a raw material, and adopting a free radical reaction to synthesize a compound III; 2) generating a compound IV from the compound III obtained in the step 1) and tert-butyl carbazate under the action of a sodium hydroxide water solution (50%) and a phase transfer catalyst TEAB; 3) generating a compound V from the compound IV obtained in the step 2) under the action of EA/HCl; and 4) generating a compound I from the compound V obtained in the step3) under the action of triethylamine and DDQ. The problems that in the prior art, the intermediates are unstable, and process amplification is difficult are solved. The shortages that the reaction conditions are severe, and the requirements on equipment and operators are very high, and the overall reaction yield is low are overcome. The synthesis method has the advantages of mild reaction conditions, high yield in each step, simple post-treatment, easiness in operation and suitability for process amplification.
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Paragraph 0014; 0045-0048
(2020/11/26)
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- INHIBITORS OF PI3 KINASE
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The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein Q, X1, X2, R1 and Z are as defined herein.
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Page/Page column 102
(2010/01/12)
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- USE OF TRIFLUOROMETHYL SUBSTITUTED BENZAMIDES IN THE TREATMENT OF NEUROLOGICAL DISORDERS
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The invention relates to methods of using the compounds of the invention, including trifluoromethyl substituted benzamide compounds and salts thereof, as well as pharmaceutical compositions comprising the same, in the treatment of Eph receptor-related (e.g., neurological) injuries and disorders. The invention also relates to modulating the activity of an Eph receptor in a cell, stimulating neural regeneration, and reversing neuronal degeneration, by administering a compound of the invention to a cell or subject in an effective amount.
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Page/Page column 40
(2008/06/13)
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- Trifluoromethyl substituted benzamides as kinase inhibitors
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The invention relates to trifluoromethyl substituted benzamide compounds of the formula I, pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases, especially of ephrin receptor kinases, and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.
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Page/Page column 22
(2008/06/13)
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- PHTHALAZINE DERIVATIVES FROM AROMATIC ALDAZINES
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A Lewis acid mediated synthesis of phthalazine derivatives II and III from aromatic aldazines I is reported.
- Robev, Stefan K.
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p. 345 - 348
(2007/10/02)
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