JAMES M. RENGA,GREGORY T. WHITEKER,CHRISTOPHER GALLIFORD,PETER LEE JOHNSON
申请号：
ARP130104694
公开号：
AR093977A1
申请日:
2013.12.13
申请国别(地区):
AR
年份:
2015
代理人:
摘要：
Claim 1: A process for the preparation of a 4-amino-5-fluoro-3-chloro-6-picolinate of the formula (1) wherein R¹ represents C₁₋₄ alkyl,cyclopropyl, C₂₋₄ alkenyl or phenyl substituted with from 1 to 4 substituents independently selected from the halogen, C₁₋₄ alkyl,C₁₋₄ haloalkyl,C₁₋₄ alkoxy or C₁₋₄ and R² haloalkoxy represents C₁₋₁₂ alkyl or a substituted or unsubstituted C₇₋₁₁ arylalkyl, comprising the following steps: a) contact trifluoroacetic acid with p-methoxyaniline in the presence of a triarylphosphine and a trialkylamine base in carbon tetrachloride solvent to produce an acetimidoyl chloride of the formula (2)；b) contact the acetimidoyl chloride of the formula (2) with a 3,3-dialkoxypropyl-1-ino (formula (3)) where R³ represents the C₁₋₄ alkyl,In the case of copper iodide (I),an alkali metal iodide and an alkali metal phosphate in a polar aprotic solvent to produce an (imino) pent-2-ino dialkyl acetal of the formula (4) where R³ is as defined above； c) cycling the (imino) pent-2-ino dialkyl acetal of the formula (4) with an amine of the formula (5) where R¹ is as defined above, in the presence of an inorganic alkali metal base in a polar solvent aprotic at a temperature from about room temperature to around 100 ° C to produce a 4- (4-methoxyphenyl) amino-5-fluoro-6-pyridine (substituted) -2-dialkyl acetal of the formula (6) where R¹ and R³ are as were defined above；(d) Clorar EL 4 - (4-methylfenilo) amino-5-fluoro-6-piridina (alternative) - 2-diacquilo acadel de la form (6) con 1, 3-dichloro-5, 5-dimethydatzolidin-2, 4. 4-amino-5-fluoro-3-chloro-6-piridina (substitute) - 2-diacquilo acadel is produced with a polar solvent, and R1 and R3 are protected from the formula (8), as described above； (e) Unprotected and hydrogenated 4-amino-5-fluoro-3-chloro-6-piridina (replaced) - 2-diacquilo acadel (protected) and a mineral acid in a polar solvent to produce R1 in the above formula (9) of 4-amino-5-fluoro-3-chloro-6-picyclohexane (replaced)；f) oxidizing the 4-amin
