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    • 6. 发明授权
    • Thiophene derivatives and methods for producing the same
    • 噻吩衍生物及其制备方法
    • US4792612A
    • 1988-12-20
    • US171388
    • 1988-03-21
    • Hiroshi GodaMasao KawamuraKunioki KatoMakoto Sato
    • Hiroshi GodaMasao KawamuraKunioki KatoMakoto Sato
    • C07D333/22C07D333/28C07D333/34C07D333/38C07D333/44
    • C07D333/44C07D333/22C07D333/28C07D333/34C07D333/38
    • Novel compounds, 2-(.alpha.-alkoxyimino)ethylthiophenes are susceptible to electrophilic substitution reactions, and the acetylation, nitration, sulfonation and halogenation of the compounds provide 5-acetyl-2-(.alpha.-alkoxyimino)ethylthiophenes, 5-nitro-2-(.alpha.-alkoxyimino)ethylthiophenes, 5-(.alpha.-alkoxyimino)ethyl-2-thiophenesulfonic acid and 5-halo-2-(.alpha.-alkoxyimino)ethylthiophenes, respectively.The hydrolysis of 5-acetyl-2-(.alpha.-alkoxyimino)ethylthiophenes readily provides a known compound, 2,5-diacetylthiophene which is an important intermediate for the production of medicines, whereas the haloform reaction provides novel compounds, 5-(.alpha.-alkoxyimino)ethyl-2-thiophenecarboxylic acids, the hydrolysis of which compounds readily provides a known compound, 5-acetyl-2-thiophenecarboxylic acids, an important intermediate for the production of medicines.The hydrolysis of 5-(.alpha.-alkoxyimino)ethyl-2-thiophenesulfonic acids and their salts provide novel 5-acetyl-2-thiophenesulfonic acid and its salts, respectively.Novel compounds, 2-(.alpha.-alkoxyimino)ethylthiophenes are obtained either by 0-alkylation of 2-acetylthiophene oxime or by directly reacting 2-acetylthiophene with an 0-alkylhydroxylamine.
    • 新化合物2-(α-烷氧基亚氨基)乙基噻吩对亲电取代反应敏感,化合物的乙酰化,硝化,磺化和卤化提供5-乙酰基-2-(α-烷氧基亚氨基)乙基噻吩,5-硝基-2- (α-烷氧基亚氨基)乙基噻吩,5-(α-烷氧基亚氨基)乙基-2-噻吩磺酸和5-卤代-2-(α-烷氧基亚氨基)乙基噻吩。 5-乙酰基-2-(α-烷氧基亚氨基)乙基噻吩的水解容易提供已知的化合物,2,5-二乙酰基噻吩,其是制备药物的重要中间体,而卤代反应提供新化合物5-(α- 烷氧基亚氨基)乙基-2-噻吩羧酸,其中哪些化合物的水解容易提供已知化合物5-乙酰基-2-噻吩羧酸,这是生产药物的重要中间体。 5-(α-烷氧基亚氨基)乙基-2-噻吩磺酸及其盐的水解分别提供新的5-乙酰基-2-噻吩磺酸及其盐。 通过2-乙酰基噻吩肟的O-烷基化或通过使2-乙酰基噻吩与O-烷基羟胺直接反应得到2-(α-烷氧基亚氨基)乙基噻吩的新型化合物。
    • 9. 发明授权
    • Novel thiophene derivatives and methods for producing the same
    • 新型噻吩衍生物及其制备方法
    • US5101049A
    • 1992-03-31
    • US569540
    • 1990-08-20
    • Hiroshi GodaMasao KawamuraKunioki KatoMakoto Sato
    • Hiroshi GodaMasao KawamuraKunioki KatoMakoto Sato
    • C07D333/22C07D333/28C07D333/34C07D333/38C07D333/44
    • C07D333/38C07D333/22C07D333/28C07D333/34C07D333/44
    • Novel compounds, 2-(.alpha.-alkoxyimino)ethylthiophenes are susceptible to electrophilic substitution reactions, and the acetylation, nitration, sulfonation and halogenation of the compounds provide 5-acetyl-2-(.alpha.-alkoxyimino)ethylthiophenes, 5-nitro-2-(.alpha.-alkoxyimino)ethylthiophenes, 5-(.alpha.-alkoxyimino)ethyl-2-thiophenesulfonic acid and 5-halo-2-(.alpha.-alkoxyimino)ethylthiophenes, respectively.The hydrolysis of 5-acetyl-2-(.alpha.-alkoxyimino)ethylthiophenes readily provides a known compound, 2,5-diacetylthiophene which is an important intermediate for the production of medicines, whereas the haloform reaction provides novel compounds, 5-(.alpha.-alkoxyimino)ethyl-2-thiophenecarboxylic acids, the hydrolysis of which compounds readily provides a known compound, 5-acetyl-2-thiophenecarboxylic acids, an important intermediate for the production of medicines.The hydrolysis of 5-(.alpha.-alkoxyimino)ethyl-2-thiophenesulfonic acids and their salts provide novel 5-acetyl-2-thiophenesulfonic acid and its salts, respectively.Novel compounds, 2-(.alpha.-alkoxyimino)ethylithiophenes are obtained either by 0-alkylation of 2-acetylthiophene oxime or by directly reacting 2-acetylthiophene with an 0-alkylhydroxylamine.
    • 新化合物2-(α-烷氧基亚氨基)乙基噻吩对亲电取代反应敏感,化合物的乙酰化,硝化,磺化和卤化提供5-乙酰基-2-(α-烷氧基亚氨基)乙基噻吩,5-硝基-2- (α-烷氧基亚氨基)乙基噻吩,5-(α-烷氧基亚氨基)乙基-2-噻吩磺酸和5-卤代-2-(α-烷氧基亚氨基)乙基噻吩。 5-乙酰基-2-(α-烷氧基亚氨基)乙基噻吩的水解容易提供已知的化合物,2,5-二乙酰基噻吩,其是制备药物的重要中间体,而卤代反应提供新化合物5-(α- 烷氧基亚氨基)乙基-2-噻吩羧酸,其中哪些化合物的水解容易提供已知化合物5-乙酰基-2-噻吩羧酸,这是生产药物的重要中间体。 5-(α-烷氧基亚氨基)乙基-2-噻吩磺酸及其盐的水解分别提供新的5-乙酰基-2-噻吩磺酸及其盐。 通过2-乙酰基噻吩肟的O-烷基化或通过使2-乙酰基噻吩与O-烷基羟胺直接反应,得到2-(α-烷氧基亚氨基)乙基噻吩类化合物。