HCID 86614262, compound → HCID 11635499, compound

Participants

Reaction Steps

0.14 g of tert-butyl (2-{[(1R)-1-(4-chlorobenzyl)-2-(3-{cyclohexyl[(diethylamino)carbonyl]amino}-8-azabicyclo[3.2.1]oct-8-yl)-2-oxoethyl]amino}ethyl)-carbamate is placed in 1.1 ml of 2N hydrochloric acid in diethyl ether. The reaction medium is stirred at ambient temperature for 1 h. Trituration, rinsing with diethyl ether and filter-drying of the precipitate obtained are carried out. The salt thus obtained is chromatographed on silica gel, elution being carried out with a 98/2/0.2 and then 95/5/0.5 mixture of dichloromethane, methanol and aqueous ammonia. 0.05 g of N-{8-[N-(2-aminoethyl)-4-chloro-D-phenylalanyl]-8-azabicyclo[3.2.1]oct-3-yl}-N-cyclohexyl-N′,N′-diethylurea hydrochloride is obtained.

Provenance & Evidence