1-PIPERIDIN-4-YL-AZEPANE synthesis

Yield:-

Reaction Conditions:

with hydrogenchloride in 1,4-dioxane;diethyl ether at 20; for 16 h;

Steps:

C-9

1.23 g (4.4 mmol) tert-butyi 4-perhydroazepin-l-yl-piperidine-l-carboxylate are dissolved in 4 mL diethyl ether and the solution is combined with 8 mL (6.3 eq, 4 M in dioxane) hydrochloric acid. After 16 h stirring at RT all the volatile constituents are eliminated in vacuo and the residue is washed with diethyl ether. After drying in vacuo 1.04 g of crude l-piperidin-4-yl-perhydroazepine hydrochloride are obtained, which are used without further purification.

References:

WO2008/77885,2008,A2 Location in patent:Page/Page column 25