Title:
エンド-ノルトロピンの調整方法とこれに用いる中間物としての8-ベンジル-ノルトロパン-3-オン-パークロレートおよびその調整方法
Document Type and Number:
Japanese Patent JP3552977
Kind Code:
B2
Abstract:
Preparation of endo-nortropine (I) comprises a 2-step treatment of new 8-benzylnortropan-3-one-perchlorate (II) with catalytically activated hydrogen Preparation of endo-nortropine (I) comprises a 2-step treatment of 8-benzylnortropan-3-one-perchlorate (II) with catalytically activated hydrogen. The method comprises: (a) pre-hydrogenation of (II) in an aqueous suspension at atmospheric pressure and at room temperature using a palladium catalyst; (b) retrieving the catalyst at the end of the reaction by filtration; (c) sending the filtrate over an anion exchanger; and (d) treating by turbulently rotating the alkaline reacting solution with Raney Nickel activated hydrogen at atmospheric pressure and room temperature at 100-1500 rotations per minute. Independent claims are also included for the following: (1) preparation of (II) comprising: (i) reacting dimethoxytetrahydrofuran, benzylamine and acetone dicarboxylic acid in an aqueous solution using the known Robinson-Schoepf method; and (ii) adding an equimolar amount of perchloric acid at room temperature to precipitate (II); (2) (II) prepared as in (1).
Inventors:
Rolf Sachse
Albert Shoup
Albert Shoup
Application Number:
JP2000016369A
Publication Date:
August 11, 2004
Filing Date:
January 26, 2000
Export Citation:
Assignee:
Dr. R. Pfleger Chemische Fabrik GmbH
International Classes:
B01J25/02; C07B61/00; C07D451/06; (IPC1-7): C07D451/06; B01J25/02
Domestic Patent References:
| JP57028085A |
Other References:
Tetrahedron Letters ,1989年,30/30,3977-3980
Attorney, Agent or Firm:
Yoshihiro Morimoto