| 摘要 |
Preparation of 4-aminobut-2-enolide compound (I) comprises reacting 5H-furan-2-one compound (II) with an amine compound (III). Preparation of 4-aminobut-2-enolide compound of formula (I) comprises reacting 5H-furan-2-one compound of formula (II) with an amine compound of formula (R 1>-NH-CH 2-A) (III). R 1> : H, (halo)alkyl, (halo)alkenyl, alkynyl, cycloalkyl, halocycloalkyl, alkoxy, alkoxyalkyl, (halo)cyclodialkyl or arylalkyl; R 2> : alkyl, aryl or arylalkyl; Z : H, alkali metal or alkaline earth metal; A : pyrid-2-yl, pyrid-4-yl or pyrid-3-yl (all optionally substituted by F, Cl, Br, CH 3, CF 3or CF 3O (at 6th position)), pyridazin-3-yl (optionally substituted by Cl or CH 3(at 6th position)), and pyrazin-3-yl, 2-chloro-pyrazin-5yl or 1,3-thiazol-5-yl (all optionally substituted by Cl or CH 3(at 2nd position)), or pyrimidinyl, pyrazolyl, thiophenyl, oxazolyl, isoxazolyl, 1,2,4-oxadiazolyl, isothiazolyl, 1,2,4-triazolyl or 1,2,5-thiadiazolyl (all optionally substituted by F, Cl, Br, CN, NO 2, (1-4C)-alkyl (optionally substituted by F and/or Cl), 1-3C-alkylthio (optionally substituted by F and/or Cl), (1-3C)-alkylsulfonyl (optionally substituted by F and/or Cl)), or substituted pyridine moiety of formula (a); and X : halo, alkyl or haloalkyl; and Y 1> : halo, alkyl, haloalkyl, haloalkoxy, azido or cyan. Independent claims are included for: (1) the preparation of an oxo ester compound of formula (R 3>O-C(=O)-CH 2-C(=O)-O-CH 2-C(=O)-OR 4>) (V) comprising reacting a potassium substituted ester compound of formula (R 3>O-C(=O)-CH 3-C(=O)-OK) (IV) with chloroacetic acid alkylester of formula (Cl-CH 3-C(=O)-OR 4>) (VI), preferably chloroacetic acid ethyl ester; and (2) a 5H-furan-2-one compound (II) of formula (IIa) or (IIb). R 2> : alkyl, preferably CH 3, aryl or arylalkyl; Z : alkali metal or alkaline earth metal, preferably Na; R 3> : alkyl, preferably C 2H 5, cycloalkyl, haloalkyl, aryl or arylalkyl; and R 4> : (cyclo)alkyl, haloalkyl, aryl or arylalkyl. [Image] [Image] [Image]. |
