Synthesis of tricyclo [3.3.1.13,7]dec-2-yl[r-(r*r*)]-3-...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/20 (2006.01) C07C 271/20 (2006.01)

Patent

CA 2123006

-12- ABSTRACT Process for the preparation of tricyclo[3.3.1.13,7]- dec-2-yl- [R-(R*,R*)]-3-(1H-indol-3-ylmethyl)-3-methyl- 4,9-dioxo-7,11-diphenyl-10-oxa-2,5,8-triazaundecanate. The present invention provides a process for the preparation of tricyclo[3.3.1.13,7]dec-2-yl[R-(R*,R*)]- 3-(1H -indol-3-ylmethyl)-3-methyl-4,9-dioxo-7,11- diphenyl-10-oxa-2,5,8-triazaundecanate, which is an important key compound for the preparation of a new class of CCK inhibitors, wherein N-[(benzyloxy)- carbonyl]-(R)-.beta.-amino-1-azido-2-phenylethane is hydrogenated, subsequently, by means of carbon dioxide, N.beta.-[(benzyloxy)-carbonyl]-(R)-.beta.-amino-2-phenylethylamine carbonate is precipitated out and this is coupled by the carbodiimide process with N-[(2-adamantyloxy)- carbonyl]-.alpha.-methyl-R-tryptophane.

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