| 摘要 |
Fused piperazin-2-one derivatives are prepared by hydrogenating with hydrogen in the presence of a hydrogenation catalyst and a specified compound; and adding a copper, iron or vanadium compound, where the hydrogenating and adding steps may take place simultaneously or successively. Preparation of fused piperazin-2-one derivatives of general formula (I), includes hydrogenating with hydrogen in the presence of a hydrogenation catalyst and a compound of formula (II); and adding a copper, iron or vanadium compound, where the hydrogenating and adding steps may take place simultaneously or successively. R 1> : a group from Cl, F, Br, methanesulfonyl, ethanesulfonyl, trifluoromethanesulfonyl, para-toluene-sulfonyl, CH 3S(=O) or phenylS(=O); R 2> : H or 1-3C alkyl; R 3> : H or a group from optionally substituted 1-12C alkyl, 2-12C alkenyl, 2-12C alkynyl or 6-14C aryl, or a group from optionally substituted and/or bridged 3-12C cycloalkyl, 3-12C cycloalkenyl, 7-12C polycycloalkyl, 7-12C polycycloalkenyl, 5-12C spirocycloalkyl or saturated or unsaturated 3-12C heterocycloalkyl, which contains 1-2 heteroatoms; R 4>, R 5> : H or optionally substituted 1-6C alkyl, or together a 2- to 5-membered alkyl bridge, which may contain 1-2 heteroatoms; A 1, A 2 : -CH= or -N=;and R 6> : 1-4C alkyl. R 4> and R 3> or R 5> and R 3> together denote a saturated or unsaturated C3-C4-alkyl bridge, which may optionally contain 1 heteroatom. An independent claim is also included for a compound of the formula (III). R 1>-R 5> : as defined above. [Image] [Image]. |
