1433507 Pharmaceutically active cyclic nucleotides TAKEDA YAKUHIN KOGYO KK 15 May 1973 [15 May 1972] 23035/73 Heading C2P [Also in Division A5] Novel nucleotides of Formula I and pharmaceutically acceptable salts thereof, where R is C 1-6 alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, aryl, aralkyl, di-(C 1-6 alkyl) amino, heterocyclic, halogen or RSP1/SPA- where RSP1/SP is C 1-6 alkyl, C 2-6 alkenyl, C 3-6 cycloalkyl, aryl or aralkyl and A is S, O or NH and R (except when halogen) and RSP1/SP may have one or more substituents selected from C 1-6 alkyl and alkoxy, C 2-6 alkenyl and alkenyloxy and C 3-6 cycloalkyl and cycloalkoxy, may be prepared by cyclizing the corresponding 5SP1/SP-monoester (or an ester thereof which may be de-esterified by a base) and optionally forming a salt. The 5SP1/SP-monoesters required as starting materials may be prepared by reacting the corresponding 2-substituted nucleoside with pyrophosphoryl chloride and optionally forming a salt. 2-n-Butylaminoadenosine-5SP1/SP-monophosphate ammonium salt is prepared by reacting 2 - chloroadenosine - 5SP1/SP - monophosphate ammonium salt with n-butylamine. The nitrophenyl esters of 2-methyl- and 2-chloroadenosine - 5SP1/SP - monophosphate tributylammonium salt are obtained by esterification with nitrophenol. The compounds of Formula I may be used as the active ingredients in conventional pharmaceutical compositions, optionally together with inositol.
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