- Synthesis method of 1H-pyrrolo[2,3-b]pyridine-2-boronic acid pinacol ester
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The invention discloses a synthesis method of 1H-pyrrolo[2,3-b]pyridine-2-boronic acid pinacol ester, and belongs to the field of medicinal chemistry. The synthesis method comprises the following steps: reacting 7-azaindole serving as a raw material with di-tert-butyl dicarbonate to synthesize 1H-pyrrolo[2,3b]pyridine-1-carboxylic acid tert-butyl ester, reacting the 1H-pyrrolo[2,3b]pyridine-1-carboxylic acid tert-butyl ester with n-butyl lithium and 1,2-dibromotetrafluoroethane at low temperature to synthesize 2-bromo-1H-pyrrolo[2,3-b]pyridine, synthesizing 2-bromo-1H-pyrrolo[2,3-b]pyridine-1-carboxylic acid tert-butyl ester, removing the protective group to obtain 2-bromo-1H-pyrrolo[2,3-b]pyridine, and reacting 2-bromo-1H-pyrrolo[2,3-b]pyridine with bi-pinacol borate under the catalytic action of transition metals to obtain the target product. The raw materials and reagents are cheap and easy to obtain, reaction conditions are mild, the safety is high, the cost is low, and the preparation method is easily applied to industrial batch production.
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Paragraph 0043; 0049; 0051
(2021/01/11)
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- COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS
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Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
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Page/Page column 98-99
(2009/12/28)
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