Title:
PRODUCTION OF DIFLUOROLACTONES
Document Type and Number:
Japanese Patent JP3692553
Kind Code:
B2
Abstract:
PURPOSE: To efficiently and readily obtain a difluorolactone containing two fluorine atoms at the 7-position useful as an intermediate for synthesizing medicines, agrochemicals or difluoroprostaglandins.
CONSTITUTION: This compound of formula I (R1, R2, R3 and R4 are each independently H, a halogen, protected OH, NH2 or CO2H or nR1, nR6 or any two selected from R3 and R4 are mutually bonded to form a ≤10C bifunctional hydrocarbon group and other R1 to R4 are independently H, a halogen, etc.; (n) is an integer of 0-10) is obtained by fluorinating a lactone of formula II with an electrophilic fluorinating agent such as N-fluorosulfonimide under basic conditions of Li in the presence of a metal compound reaction agent such as B or Mg. In the reaction, 1 pt.wt. of the lactone is reacted with 2-10 pts.wt. of the electrophilic fluorinating agent in the presence of 2-10 pts.wt. of the base and 0.1-10 pts.wt. of the metal compound reaction agent in 10-100 pts.wt. of an inert solvent such as diethyl ether at -8°C to +40°C.
Inventors:
Yasushi Matsumura
Takashi Nakano
Yoshitomi Morisawa
Takashi Nakano
Yoshitomi Morisawa
Application Number:
JP28385794A
Publication Date:
September 07, 2005
Filing Date:
November 17, 1994
Export Citation:
Assignee:
Asahi Glass Co., Ltd.
International Classes:
C07D307/32; C07B39/00; C07D305/12; C07D307/33; C07D307/935; C07D309/30; C07D311/20; C07D311/94; C07D313/00; C07D407/12; C07F7/18; (IPC1-7): C07D307/935; C07B39/00; C07D307/33; C07D407/12; C07F7/18
Domestic Patent References:
| JP56501319A |
Other References:
DIFFERDING E.,Selective mono-and difluorination of enonlates",Tetrahedron Letters,1991年, 32/15,p1779-1782
Attorney, Agent or Firm:
Yoko Hasegawa
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