C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 451/12 (2006.01) A61K 31/46 (2006.01) C07D 451/06 (2006.01)
Patent
CA 2495988
This invention provides a method for preparing a hydroxyalkyl tropane ester, comprising: (a) contacting a tropane and 1,1'-carbonyldiimidazole to produce an activated tropane ester; (b) contacting the activated tropane ester with an excess of an alkanediol to form a reaction mixture; and (c) maintaining the reaction mixture at a temperature and for a sufficient time for the activated tropane ester to react with the alkanediol to form the corresponding hydroxyalkyl tropane ester. This method may be used to produce hydroxyalkyl derivatives of tropanes such as benzoylecgonine, ecgonine and ecgonidine.
La présente invention concerne un procédé de préparation d'un hydroxyalkyl tropane ester. Ledit procédé consiste: (a) à mettre en contact un tropane et du 1,1'-carbonyldiimidazole afin de produire un tropane ester activé; (b) à mettre en contact le tropane ester activé avec un excès d'alcanediol afin de former un mélange réactionnel; et (c) à conserver le mélange réactionnel à une certaine température et pendant une durée suffisante afin que le tropane ester activé réagisse avec l'alcanediol afin de former l'hydroxyalkyl tropane ester correspondant. Ledit procédé peut être utilisé afin de produire des dérivés hydroxyalkylés de tropanes tels que benzoylecgonine, ecgonine et ecgonidine.
Hayes James P.
Lewin Anita H.
Zhong Desong
Entropin Inc.
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