Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1999-04-13
2000-03-21
Chang, Ceila
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C07D40106
Patent
active
060404493
ABSTRACT:
In the production of fluorine-containing 1,4-disubstituted piperidine derivatives by the reaction of a carboxylic acid of formula where Ar represents aryl or heteroaryl and R.sup.10 represents C.sub.3 -C.sub.6 cycloalkyl in which up to 4 hydrogen atoms are substituted with fluorine or C.sub.3 -C.sub.6 cycloalkyl having 1 to 2 protected or unprotected hydroxyl or oxo groups, or a reactive derivative thereof, with a piperidine derivative of formula [IV] as defined in the specification, especially useful results are obtained using 4-amino-1-(6-aminopyridin-2-ylmethyl)piperidine or a salt thereof, e.g., trihydrochloride, as the piperidine derivative.
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Japanese language publication "Seitai no Kagaku" (biochemistry), vol. 42(5), p. 380-385, 1991 and partial English translation.
Chem. Pharm. Bull., vol. 32, No. 3, (1984), SUGAI, Saburo, et al., "Studies on Spasmolytics I. Synthesis and Spasmolytic . . . piperidines", p. 967-976.
Chem. Pharm. Bull., vol. 32, No. 3, (1984), SUGAI, Saburo, et al., "Studies on Spasmolytics. II. Synthesis . . . Compounds", p. 997-985.
Chem. Pharm. Bull. vol. 32, No. 3, (1984), SUGAI, Saburo, et al., "Studies on Spasmolytics. III. Synthesis . . . Salts", p. 1126-1134.
Chem. Pharm. Bull. vol. 33, No. 2, (1985), Yoshida, Seiichiro, et al., "Structure-Activity Relationship . . . piperidine Deriviatives", p. 818-822.
Kawakami Kumiko
Nishikibe Masaru
Nomoto Takashi
Ohsawa Hirokazu
Ohwaki Kenji
Banyu Pharmaceutical Co Ltd
Chang Ceila
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