| 摘要 |
<p>PURPOSE:To obtain the titled compound useful as an antibacterial agent can be produced by reacting a specific 2-(5-fluoronicotinoyl)-acetic acid derivative or its salt with an acetal of a specific N,N-disubstituted formamide. CONSTITUTION:The objective compound of formula III (R<1> is protecting group) or its salt can be produced by reacting (A) the compound of formula I (R<1a> is protecting group; R<2> is halogen, hydroxyl, azido, alkoxy, alkylthio, 3-amino-1- pyrrolidinyl, 1-piperazinyl, etc.; X is H or F) or its salt with (B) the compound of formula II (R<3> and R<4> are alkyl or cycloaralkyl or R<3> and R<4> together form an alkylene; R<5> and R<6> are alkyl or R<5> and R<6> together with N form a heterocyclic group in the presence or absence of a solvent, usually at 0-150 deg.C for 5min-3hr, and if necessary, subjecting the product to deprotecting, etc. The amount of the compound B is usually >=1mol per 1mol of the compound A.</p> |
