| 摘要 |
<p><P>PROBLEM TO BE SOLVED: To provide a method for producing a 3-cyclopropylaminomethyl-4-fluoropyrrolidine derivative as an intermediate for a quinolonecarboxylic acid derivative and its salt and hydrate that are safe and express strong antibacterial activities. <P>SOLUTION: The method for producing the 3-cyclopropylaminomethyl-4-fluoropyrrolidine derivative of general formula(6)( wherein, R2 is H or F ) comprises the following process: A (4-hydroxypyrrolidin-3-yl)methanol derivative is brominated to form a 3-bromomethyl-4-hydroxypyrrolidine derivative, the 4-site hydroxy group of which is fluorinated to form a 3-bromomethyl-4-substituted pyrrolidine derivative, which is then reacted with a cyclopropylamine derivative to form a 3-cyclopropylaminomethyl-4-fluoropyrrolidine derivative followed by eliminating the protecting group for the amino group. <P>COPYRIGHT: (C)2005,JPO&NCIPI</p> |
