Patent ID: 6222039
Filing Date: 2001-04-24
Classification: C07D

Abstract:
A process for producing a compound of formula (IV) ##STR17##wherein R.sup.1 is lower alkyl or lower cycloalkyl; R.sup.2 is a 5- or 6-membered N-heterocyclic ring wherein (a) the ring is covalently bonded to the remainder of the compound via a linking N atom, (b) the ring contains 0, 1 or 2 additional hetero groups as ring members, selected from the group consisting of N, O and/or S, SO or SO.sub.2, (c) both ring atoms adjacent to the linking N atom are C, one or both of which are substituted by oxo, (d) the ring is either optionally benz-fuzed or optionally substituted by lower allyl or oxo on one or more C atoms non-adjacent to the linking N atom; (e) the ring is optionally substituted by lower alkyl on one or more N atom(s) non-adjacent to the linking N atom by lower alkyl; and R.sup.3 is a saturated 5- to 7-membered monocyclic N-heterocyclic ring which is attached to the remainder of the compound of formula IV via the N-atom and optionally contains one additional hetero group selected from NR.sup.4 and O as a ring member; and R.sup.4 is hydrogen, lower alkyl, aryl, aralkyl or a protecting group, comprising:a) reacting a compound of formula (I) ##STR18##with a cyclic amine HR.sup.3 yielding a compound of formula (V) ##STR19##b) oxidizing the hydroxyl group in a compound of formula (V) yielding a compound of formula VI ##STR20##c) introducing a hydroxyl amine at the hydroxyl of the compound of formula (VI), yielding the compound of formula (IV).