NOVEL METHOD FOR PRODUCING 1,4-DIHYDRO-4-OXONAPHTYRIDINE DERIVATIVE OR SALT THEREOF

• Main Authors: KITAYAMA ISAO, NARITA HIROKAZU, NAGAKI HIDEYOSHI, KONISHI YOSHINORI, TODO YOZO, SHINAGAWA MIKAKO, NANUN KATSUYUKI, TAKANO SHUNTARO, SAIKAWA ISAMU, SANTO TETSUO
• Format: Patent
• Language: English
• Published: 19.12.1986
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

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 is protecting group) or its salt can be produced by reacting (A) the compound of formula I (R is protecting group; R 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 and R are alkyl or cycloaralkyl or R and R together form an alkylene; R and R are alkyl or R and R 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.