Preparation method of poly-substitution 6-fluorine picolinic acid
The invention discloses a preparation method of poly-substitution 6-fluorine picolinic acid. The preparation method comprises the following steps: performing diazotization on the poly-substitution 2-amino-6-picoline and a diazotized agent; performing a reaction on a fluorinating agent to generate the poly-substitution 2-amino-6-fluoride pyridine; performing an oxidizing reaction on the poly-substitution 6-picoline-2-fluoride pyridine and an oxidizing agent to obtain the poly-substitution 6-fluorine picolinic acid. The invention provides a novel initial raw material for preparing poly-substitution 6-fluorine picolinic acid, and correspondingly provides a novel reaction path and process. The poly-substitution 2-amino-6-picoline is taken as the initial raw material has the advantages of low cost and readily-available; the prepared 6-fluorine picolinic acid has the advantages of simple process, low requirement on reaction conditions, high security performance, high product yield and purityand easiness in realizing scale production.
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Paragraph 0021-0023; 0025-0027
(2018/09/08)
SAR of 3,4-dihydropyrido[3,2-d]pyrimidone p38 inhibitors
Development for a class of potent 3,4-dihydropyrido(3,2-d)pyrimidone inhibitors of p38a MAP kinase is described. Modification of N-1 aryl and C-6 arylsulfide in 3,4-dihydropyrido(3,2-d)pyrimidone analogues for the interaction with the hydrophobic pockets
Liu, Luping,Stelmach, John E.,Natarajan, Swaminathan R.,Chen, Meng-Hsin,Singh, Suresh B.,Schwartz, Cheryl D.,Fitzgerald, Catherine E.,O'Keefe, Stephen J.,Zaller, Dennis M.,Schmatz, Dennis M.,Doherty, James B.
p. 3979 - 3982
(2007/10/03)
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