METHOD OF PRODUCING INTERMEDIATE PRODUCT FOR SYNTHESIS OF mu OPIOID RECEPTOR ANTAGONISTS Russian patent published in 2012 - IPC C07D451/02 

Abstract RU 2469035 C2

FIELD: chemistry.

SUBSTANCE: invention relates to methods of producing 3-endo(8-azabicyclo[3.2.1]oct-3-yl)benzamide of formula 1 . The methods are realised via hydrogenation of an intermediate product, amine-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide of formula 3, in the presence of hydrochloric or trifluoroacetic acid, where the amine-protective group is a removable by catalytic hydrogenation. The invention also relates to intermediate compounds 2, 3 and 5, a method of producing a compound of formula 3 and a method of increasing stereospecifity for endo-orientation of a 3-endo(8-azabicyclo[3.2.1]oct-3-yl)benzamide sample.

EFFECT: improved methods of producing 3-endo(8-azabicyclo[3,2,1]oct-3-yl)benzamide.

14 cl, 1 dwg, 4 ex

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RU 2 469 035 C2

Authors

Kol'Son P'Er-Zhan

Juj In

Long Dehniel D.

Stergiades Ioanna

Dates

2012-12-10Published

2008-07-15Filed