| 摘要 |
3-Thiazolyl-4-hydroxy-5,6-dihydropyrone or 3-thiazolyl-4-hydroxy-tetrahydropyridone derivatives (I) are new. 3-Thiazolyl-4-hydroxy-5,6-dihydropyrone or 3-thiazolyl-4-hydroxy-tetrahydropyridone derivatives of formula (I) are new. Het = 5-membered nitrogen-containing heterocycle of the thiazole series (optionally substituted (os) by halo, alkyl, alkoxy, alkenyloxy, haloalkyl, haloalkoxy, haloalkenyloxy, CN, NO2, alkylthio, alkylsulfinyl, alkylsulfonyl, os phenyl or os phenoxy); W = O or N-D; A = H, alkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl or alkylthioalkyl (all os by halo), saturated or unsaturated cycloalkyl (os) (optionally having at least one ring atom replaced by a heteroatom) or aryl, aralkyl or heteroaryl (all os by halo, alkyl, haloalkyl, alkoxy, haloalkoxy, CN or NO2); B' = H or alkyl; or CAB' = ring (os, saturated or unsaturated and optionally containing at least one heteroatom); D = H, alkyl, alkenyl, alkynyl, alkoxyalkyl, polyalkoxyalkyl, alkylthioalkyl, cycloalkyl (saturated or unsaturated and optionally having at least one ring atom replaced by a heteroatom), aryl, aralkyl, heteroaralkyl or heteroaryl (all os); or A + Q1 = alkanediyl (os by os alkyl or os alkoxy), in which two non-adjacent C atoms may be part of a further ring (os); or D + Q1 = group (os, saturated or unsaturated and optionally containing at least one heteroatom) completing a ring; Q1 = H, alkyl, alkoxyalkyl, cycloalkyl (os and optionally having one CH2 replaced by O or S) or phenyl (os); Q2 = H or alkyl; or CQ1Q2 = ring (os and optionally containing a heteroatom); G = H, COR1, C(L)MR2, SO2R3, P(L)R4R5, E or C(L)-NR6R7; E = metal or ammonium ion; L, M = O or S; R1 = alkyl, alkenyl, alkoxyalkyl, polyalkoxyalkyl or alkylthioalkyl (all os by halo), cycloalkyl (optionally interrupted by at least one heteroatom and os by halo, alkyl or alkoxy), or phenyl, phenylalkyl, heteroaryl, phenoxyalkyl or heteroaryloxy (all os); R2 = alkyl, alkenyl, alkoxyalkyl or polyalkoxyalkyl (all os by halo) or cycloalkyl, phenyl or benzyl (all os); R3 = alkyl, haloalkyl, phenyl (os) or benzyl (os); R4, R5 = alkyl, alkoxy, mono- or dialkylamino, alkylthio, alkenylthio or cycloalkylthio (all os by halo) or phenyl, benzyl, phenoxy or phenylthio (all os); R7, R8 = H, alkyl, cycloalkyl, alkenyl, alkoxy or alkoxyalkyl (all os by halo) or phenyl or benzyl (both os); and NR7R8 = heterocycle (optionally interrupted by O or S). Independent claims are included for: (1) Preparation of (I); and (2) New amide, ester and nitrile intermediates of formulae (II) and (XX). R8 = alkyl or H. Provided that R8 is H, when W is N-D.
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