- Cu-catalyzed oxygenation of alkene-tethered amides with O2: Via unactivated CC bond cleavage: A direct approach to cyclic imides
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The transformations of unactivated alkenes through CC bond double cleavage are always attractive but very challenging. We report herein a chemoselective approach to valuable cyclic imides by a novel Cu-catalyzed geminal amino-oxygenation of unactivated CC bonds. O2 was successfully employed as the oxidant as well as the O-source and was incorporated into alkenyl amides via CC bond cleavage for the efficient preparation of succinimide or glutarimide derivatives. Moreover, the present strategy under simple conditions can be used in the late-stage modification of biologically active compounds and the synthesis of pharmaceuticals, which demonstrated the potential application.
- Li, Junhua,Wei, Jialiang,Zhu, Bencong,Wang, Teng,Jiao, Ning
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p. 9099 - 9103
(2019/10/22)
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- AMIDOALKYLPIPERAZINYL DERIVATIVES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES
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The invention relates to novel amidoalkylpiperazinyl derivatives of tricyclic heterocyclic systems of general formula (I), wherein Z represents -NH- and X represents -S-, or Z represents -S- and X represents >C=C1 represents H or -CH3, R6 and R7 both represent H, n is an integer from 0 to 4 inclusive, G represents a cyclic amide or imide moiety, and optical isomers, geometric isomers, and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.
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Page/Page column 28; 29
(2013/03/26)
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- Synthesis and anticonvulsant properties of new mannich bases derived from 3,3-disubstituted pyrrolidine-2,5-diones. Part IV
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A library of 21 new N-Mannich bases of 3,3-diphenyl- (5a-g), 3-methyl-3-phenyl- (6a-g), and 3-ethyl-3-methylpyrrolidine-2,5-diones (7a-g) were synthesized and evaluated for their anticonvulsant activity in the maximum electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure tests after intraperitoneal injection into mice. The acute neurological toxicity was determined applying the rotarod screen. The results in mice showed that 13 compounds were effective in the MES or/and scPTZ screen. From these, seven molecules were tested in the MES seizures after oral administration in rats. The quantitative studies showed that N-[{4-(2-hydroxyethyl)-piperazin-1-yl}-methyl] -3-methyl-3-phenylpyrrolidine-2,5-dione (6c) and N-[(4-benzylpiperidin-1-yl)- methyl]-3-methyl-3-phenylpyrrolidine-2,5-dione (6f) revealed higher protection in the MES and scPTZ tests than valproic acid or ethosuximide which were used as reference antiepileptic drugs. Four compounds (5c, 6c, 6e, 6f) showed high effectiveness in the 6-Hz psychomotor seizure model of partial and therapy resistant epilepsy.
- Obniska, Jolanta,Chlebek, Iwona,Kaminski, Krzysztof
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p. 713 - 722
(2012/10/30)
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- Uncatalyzed Cationic Olefin Cyclizations of N-Vinylic α-Chloro-α-thioacetamides. Formation of β- and γ-Lactams
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N-Vinylic α-chloro-α-thioacetamides were found to cyclize without a catalyst in two different manners depending upon the nature of the substituents at the terminus of the N-vinylic bond.Thus, bis(phenylthio)-substituted enamides 8a-c cyclized in a 4-exo-trig manner to give 4-methylene-β-lactams 10a-c, whereas mono(phenylthio)-, monophenyl-, and dialkyl-substituted congeners 23a,b, 28, and 38 cyclized in a 5-endo-trig manner to give γ-lactams 26a,b, 30, and 39, respectively.The product 38 was transformed into an anticonvulsant agent ethosuximide (42).
- Ishibashi, Hiroyuki,Nakaharu, Tohru,Nishimura, Masako,Nishikawa, Atsuko,Kameoka, Chisato,Ikeda, Masazumi
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p. 2929 - 2938
(2007/10/02)
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