【药物名称】Lidorestat, EML-676, IDD-000676-01, IDD-676
化学结构式(Chemical Structure):
参考文献No.44976
标题:Methods of reducing serum glucose and triglyceride levels and for inhibiting angiogenesis using substd. indolealkanoic acids
作者:Jacot, J.; Sredy, J. (The Institutes for Pharmaceutical Discovery, Inc.)
来源:WO 0032180
合成路线图解说明:

Acetylation of 2,3,5,6-tetrafluoroaniline (I), followed by treatment of the resulting acetanilide (II) with P2S5, gave thioamide (III). Cyclization of (III) in the presence of NaH produced the benzothiazole (IV), which was subsequently hydrolyzed to amino thiophenol (V) by means of NaOH in ethyleneglycol.

合成路线图解说明:

Alkylation of 3-indolylacetonitrile (VI) with ethyl bromoacetate provided indoleacetate ester (VII). Condensation of the cyano group of (VII) with amino thiophenol (V) in hot EtOH furnished benzothiophene (VI). The ethyl ester group of (VI) was finally hydrolyzed with NaOH to the title carboxylic acid.

参考文献No.44977
标题:Substd. indolealkanoic acids
作者:Jones, J.H.; Jones, M.L.; Gunn, D.; Van Zandt, M.C. (The Institutes for Pharmaceutical Discovery, Inc.)
来源:WO 9950268
合成路线图解说明:

Acetylation of 2,3,5,6-tetrafluoroaniline (I), followed by treatment of the resulting acetanilide (II) with P2S5, gave thioamide (III). Cyclization of (III) in the presence of NaH produced the benzothiazole (IV), which was subsequently hydrolyzed to amino thiophenol (V) by means of NaOH in ethyleneglycol.

合成路线图解说明:

Alkylation of 3-indolylacetonitrile (VI) with ethyl bromoacetate provided indoleacetate ester (VII). Condensation of the cyano group of (VII) with amino thiophenol (V) in hot EtOH furnished benzothiophene (VI). The ethyl ester group of (VI) was finally hydrolyzed with NaOH to the title carboxylic acid.

参考文献No.54901
标题:Methods for lowering uric acid levels
作者:Boyd, M.; Robinson, D. (The Institutes for Pharmaceutical Discovery, Inc.)
来源:WO 0151489
合成路线图解说明:

Acetylation of 2,3,5,6-tetrafluoroaniline (I), followed by treatment of the resulting acetanilide (II) with P2S5, gave thioamide (III). Cyclization of (III) in the presence of NaH produced the benzothiazole (IV), which was subsequently hydrolyzed to amino thiophenol (V) by means of NaOH in ethyleneglycol.

合成路线图解说明:

Alkylation of 3-indolylacetonitrile (VI) with ethyl bromoacetate provided indoleacetate ester (VII). Condensation of the cyano group of (VII) with amino thiophenol (V) in hot EtOH furnished benzothiophene (VI). The ethyl ester group of (VI) was finally hydrolyzed with NaOH to the title carboxylic acid.

参考文献No.54902
标题:Compsns. containing a substd. indolealkanoic acid and an angiotensin converting enzyme inhibitor
作者:Van Zandt, M.; Sredy, J. (The Institutes for Pharmaceutical Discovery, Inc.)
来源:WO 0164205
合成路线图解说明:

Acetylation of 2,3,5,6-tetrafluoroaniline (I), followed by treatment of the resulting acetanilide (II) with P2S5, gave thioamide (III). Cyclization of (III) in the presence of NaH produced the benzothiazole (IV), which was subsequently hydrolyzed to amino thiophenol (V) by means of NaOH in ethyleneglycol.

合成路线图解说明:

Alkylation of 3-indolylacetonitrile (VI) with ethyl bromoacetate provided indoleacetate ester (VII). Condensation of the cyano group of (VII) with amino thiophenol (V) in hot EtOH furnished benzothiophene (VI). The ethyl ester group of (VI) was finally hydrolyzed with NaOH to the title carboxylic acid.

参考文献No.589335
标题:Substituted indolealkanoic acids as novel aldose reductase inhibitors
作者:Jones, J.H.; Gunn, D.; Jones, M.L.; Van Zandt, M.C.; Lavoie, D.J.; Sawicki, D.; Sredy, J.; Howard, E.; Podjarny, A.D.
来源:220th ACS Natl Meet (Aug 20 2000, Washington DC) 2000,Abst MEDI 307
合成路线图解说明:

Acetylation of 2,3,5,6-tetrafluoroaniline (I), followed by treatment of the resulting acetanilide (II) with P2S5, gave thioamide (III). Cyclization of (III) in the presence of NaH produced the benzothiazole (IV), which was subsequently hydrolyzed to amino thiophenol (V) by means of NaOH in ethyleneglycol.

合成路线图解说明:

Alkylation of 3-indolylacetonitrile (VI) with ethyl bromoacetate provided indoleacetate ester (VII). Condensation of the cyano group of (VII) with amino thiophenol (V) in hot EtOH furnished benzothiophene (VI). The ethyl ester group of (VI) was finally hydrolyzed with NaOH to the title carboxylic acid.

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