Special 3-azabicyclo[3.1.0]hexanes, method for producing and...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/52 (2006.01) A61K 31/47 (2006.01) C07D 471/04 (2006.01) C07D 471/14 (2006.01)

Patent

CA 2298509

The invention relates to novel 3-azabicyclo[3.1.0]hexanes with a doubly protected amino group in position 6, and to a method for producing the same from chloramines or bicyclic N,O acetals or bicyclic nitriles. The two protective groups on the amino group in 6 and the group on N(3) can be specifically removed. The novel 3-azabicyclo[3.1.0]hexanes with a doubly protected amino group in position 6 are suitable for manufacturing pharmaceutical products, e.g. gyrase inhibitors, which can be modified by subsequently splitting off the protective groups.

L'invention concerne de nouveaux 3-azabicyclo[3.1.0]hexanes avec un groupe amino diprotégé en position 6, et leur procédé de préparation à partir de chloramines ou de N,O-acétals bicycliques ou encore de nitriles bicycliques. Les deux groupes protecteurs sur le groupe amino en 6, ainsi que le groupe sur N(3) peuvent être éliminés de manière appropriée. Ces nouveaux 3-azabicyclo[3.1.0]hexanes avec un groupe amino diprotégé en position 6 conviennent pour fabriquer des médicaments, par exemple des inhibiteurs de la gyrase, qui peuvent être modifiés par séparation subséquente des groupes protecteurs.

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