New 6-cyclohexyl-2'-O-methyl-adenosine hydrate - has better purity and formulation characteristics than known mono:etherate

摘要

6-Cyclohexyl-2' -O-methyl-adenosine 1.5 hydrate (I) is new. USE/ADVANTAGE - (I) has the same pharcological properties as 6-cyclohexyl-2' -O-methyl-adenosine monoetherate (II) which is known from DE 3940021. Compared with this etherate, (I) is obtd. in purer form and is easier to formulate into pharmaceutical prepns. In an example, 6-Chloro-9-purinyl -2'-O-methyl-D-ribose (0.7 g) was heated in cyclohexylamine (30 ml), concentrated, chromatographed (silica gel; dichloromethane:ethanol 95:5), crystallised (dichloromethane/diethyl ether) and then recrystallised (ethanol/water) to give (I); m.pt. 88-91 deg.C.