Improvements in the chichibabin amination process

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 213/74 (2006.01) C07D 207/34 (2006.01) C07D 213/65 (2006.01) C07D 213/73 (2006.01) C07D 213/80 (2006.01) C07D 213/82 (2006.01) C07D 215/38 (2006.01) C07D 239/42 (2006.01) C07D 401/04 (2006.01)

Patent

CA 1255675

ABSTRACT OF THE DISCLOSURE In a Chichibabin amination of a nitrogen-containing heterocyclic base by sodamide in an organic solvent, the improvement comprising conducting the reaction under pressure of at least about 50 psi in the gas phase above the reaction mixture and adding ammonia to the mixture sufficient to produce a partial pressure of ammonia of at least about 5 psi in the gas phase. Preferred temperature and pressure ranges are disclosed, as are catalysts and other preferred steps for practicing the reaction. Significant results are obtained including improved and changed yields from those classically expected in Chichibabin aminations, including new compounds which are valuable intermediates in synthesis.

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