2-FLUOROCYCLOPROPYLAMINE DERIVATIVE AND ITS PRODUCTION

Japanese Patent JP3329492

B2

PURPOSE: To produce the subject compound useful as a production raw material for a quinolone derivative known as an excellent antibacterial agent on an industrial scale at a low cost by using an inexpensive 1-arylalkylamine derivative as a starting raw material and converting the raw material through intermediates including new compounds.
CONSTITUTION: The objective (1R*,2S*)-2-fluorocyclopropylamine of formula 6 is produced by carrying out dehydrative condensation reaction of a 1- arylalkylamine derivative of formula 1 (Ar is phenyl or naphthyl; R1 is alkyl or phenyl) with acetaldehyde, reacting the resultant compound of formula 2 with phosgene, etc., to obtain a compound of formula 3, reacting the compound with a compound of the formula MOY (M is alkali metal; Y1 is alkyl having 1-3 aryl groups at 1-site, alkyl, etc.) to obtain a compound of formula 4 (including new compound), adding a monofluorocarbene to obtain a compound of formula 5 (including new compound) and finally hydrolyzing the product under strongly acidic condition. In the intermediates in the above reactions, the compound of formula 7 (Y2 is alkyl) and the compound of formula 8 are new compounds.

Toro Terashima
Osamu Tamura
Yuko Kobayashi
Masaru Hashimoto
Tadashi Kato
Kazuhiko Nakatani
Yusuke Yukimoto
Tsutomu Ebata
Toshifumi Akiba
Hirofumi Kawanishi

JP24185392A

September 30, 2002

September 10, 1992

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Daiichi Pharmaceutical Co., Ltd.
Sagami Central Chemical Research Institute

C07C209/62; C07C211/37; C07C269/06; C07C271/12; C07C271/24; C07C271/34; C07C271/36; (IPC1-7): C07C271/24; C07C209/62; C07C211/37; C07C269/06; C07C271/12

JP5163212A

Miyuki Ariga (3 outside)

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