Process for Preparing Pharmaceutically Usable Substituted 5H-Pyrimido / 5,4-b / Indole-2-Carboxylic Acid Esters

摘要

Substituted 5H-pyrimido[5,4-b]indoles of Formula I IMAGE (I) wherein R2 is halogen; the oxadiazolyl group IMAGE wherein R'' is lower alkyl with up to 3 carbon atoms; C1-5-alkyl, cycloalkyl, aralkyl, or aryl; ORI, SOnRI with n being 0, 1, or 2, or IMAGE wherein RI is hydrogen, C1-5-alkyl, cycloalkyl, aralkyl, or aryl; IMAGE wherein RII and RIII are hydrogen, C1-5-alkyl, C3-5-alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; and RA is hydrogen; the oxadiazolyl group IMAGE wherein R'' is lower alkyl with up to 3 carbon atoms; halogen, nitro, ORI, SOnRI with n being 0, 1, or 2, IMAGE wherein RI is hydrogen, C1-5-alkyl, cycloalkyl, aralkyl, or aryl; IMAGE wherein RII and RIII are hydrogen, C1-5-alkyl, cycloalkyl, C3-5-alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; or PO(OR)2 wherein R is C1-5-alkyl, exhibit strong affinity for binding to benzodiazepine receptors. The novel compounds are suitable for use in psychopharmaceutical preparations.