【药物名称】Isoprofen, UP-517-03
化学结构式(Chemical Structure):
参考文献No.803986
标题:Isoprofen
作者:Blancafort, P.; Serradell, M.N.; Casta馿r, J.; Arrigoni, Martelli, E.
来源:Drugs Fut 1981,6(8),471
合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with ethyloxalyl chloride (II) by means of AlCl3 in methylene chloride gives ethyl 2-(2-isopropyl-5-indanyl)-2-oxoacetate (III), which is hydrolyzed with NaOH in refluxing ethanol to the corresponding free acid (IV). The reaction of (IV) with methylmagnesium iodide in ether yields 2-(2-isopropyl-5-indanyl)-2-hydroxypropionic acid (V), which is dehydrated with H2SO4 in refluxing dioxane affording 2-(2-isopropyl-5-indanyl)acrylic acid (VI) (1,2,4). Finally this compound is reduced with H2 over Raney-Ni or Pd/C in methanol or dioxane

合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with acetic anhydride in methylene chloride gives 2-isopropyl-5-acetylindan (VII), which by with sulfur and morpholine (A) at 140 C gives 2-(2-isopropyl-5-indanyl)acetylmorpholinothioamide (XI), which is hydrolyzed to 2-(2-isopropyl-5-indanyl)acetic acid (XII). The esterification of (XII) with ethanol - H2SO4 yields the corresponding ethyl ester (XIII), which is condensed with diethyl carbonate (XIV) by means of sodium ethoxide in refluxing ethanol affording diethyl (2-isopropyl-5-indanyl)malonate (XV), which is methylated with methyl iodide and sodium ethoxide in refluxing ethanol to give diethyl methyl-(2-isopropyl-5-indanyl)malonate (XVI). Finally this compound is hydrolyzed and decarboxylated by treatment with NaOH in refluxing hydrazine hydrate Compound (XII) can also be obtained by a Wolf-Kistner reduction of ketoacid (IV) in refluxing hydrazine hydrate

合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with acetic anhydride in methylene chloride gives 2-isopropyl-5-acetylindan (VII), which is reduced with KBH4 in methanol yielding 2-isopropyl-5-(1-hydroxyethyl)indan (VIII). The treatment of (VIII) with SOCl2 in benzene affords 2-isopropyl-5-(1-chloroethyl)indan (IX), which by reaction with NaCN in hot HMPA yields 2-(2-isopropyl-5-indanyl)propionitrile (X). Finally this compound is hydrolyzed with H2SO4 in refluxing acetic acid - water

参考文献No.803987
标题:Antiinflammatory and analgesic diastereoisomeric derivatives of indan-5-acetic acid
作者:Teulon, J.M.; et al.
来源:J Med Chem 1978,21(4),901
合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with ethyloxalyl chloride (II) by means of AlCl3 in methylene chloride gives ethyl 2-(2-isopropyl-5-indanyl)-2-oxoacetate (III), which is hydrolyzed with NaOH in refluxing ethanol to the corresponding free acid (IV). The reaction of (IV) with methylmagnesium iodide in ether yields 2-(2-isopropyl-5-indanyl)-2-hydroxypropionic acid (V), which is dehydrated with H2SO4 in refluxing dioxane affording 2-(2-isopropyl-5-indanyl)acrylic acid (VI) (1,2,4). Finally this compound is reduced with H2 over Raney-Ni or Pd/C in methanol or dioxane

合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with acetic anhydride in methylene chloride gives 2-isopropyl-5-acetylindan (VII), which is reduced with KBH4 in methanol yielding 2-isopropyl-5-(1-hydroxyethyl)indan (VIII). The treatment of (VIII) with SOCl2 in benzene affords 2-isopropyl-5-(1-chloroethyl)indan (IX), which by reaction with NaCN in hot HMPA yields 2-(2-isopropyl-5-indanyl)propionitrile (X). Finally this compound is hydrolyzed with H2SO4 in refluxing acetic acid - water

参考文献No.900215
标题:
作者:Teulon, J.M.; et al. (Hexachimie SA)
来源:BE 824522; CA 1063618; CH 603533; CH 605567; DD 117209; DD 118271; DD 123319; DE 2504689; FR 2260334; GB 1492175; JP 76125367; JP 76125368; NL 7501518; NL 7501519; US 4069326; US 4088787; US 4182896; ZA 7500707
合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with ethyloxalyl chloride (II) by means of AlCl3 in methylene chloride gives ethyl 2-(2-isopropyl-5-indanyl)-2-oxoacetate (III), which is hydrolyzed with NaOH in refluxing ethanol to the corresponding free acid (IV). The reaction of (IV) with methylmagnesium iodide in ether yields 2-(2-isopropyl-5-indanyl)-2-hydroxypropionic acid (V), which is dehydrated with H2SO4 in refluxing dioxane affording 2-(2-isopropyl-5-indanyl)acrylic acid (VI) (1,2,4). Finally this compound is reduced with H2 over Raney-Ni or Pd/C in methanol or dioxane

合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with acetic anhydride in methylene chloride gives 2-isopropyl-5-acetylindan (VII), which by with sulfur and morpholine (A) at 140 C gives 2-(2-isopropyl-5-indanyl)acetylmorpholinothioamide (XI), which is hydrolyzed to 2-(2-isopropyl-5-indanyl)acetic acid (XII). The esterification of (XII) with ethanol - H2SO4 yields the corresponding ethyl ester (XIII), which is condensed with diethyl carbonate (XIV) by means of sodium ethoxide in refluxing ethanol affording diethyl (2-isopropyl-5-indanyl)malonate (XV), which is methylated with methyl iodide and sodium ethoxide in refluxing ethanol to give diethyl methyl-(2-isopropyl-5-indanyl)malonate (XVI). Finally this compound is hydrolyzed and decarboxylated by treatment with NaOH in refluxing hydrazine hydrate Compound (XII) can also be obtained by a Wolf-Kistner reduction of ketoacid (IV) in refluxing hydrazine hydrate

合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with acetic anhydride in methylene chloride gives 2-isopropyl-5-acetylindan (VII), which is reduced with KBH4 in methanol yielding 2-isopropyl-5-(1-hydroxyethyl)indan (VIII). The treatment of (VIII) with SOCl2 in benzene affords 2-isopropyl-5-(1-chloroethyl)indan (IX), which by reaction with NaCN in hot HMPA yields 2-(2-isopropyl-5-indanyl)propionitrile (X). Finally this compound is hydrolyzed with H2SO4 in refluxing acetic acid - water

参考文献No.900216
标题:
作者:Payne, T.G. (Hexachimie SA)
来源:CH 605565
合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with ethyloxalyl chloride (II) by means of AlCl3 in methylene chloride gives ethyl 2-(2-isopropyl-5-indanyl)-2-oxoacetate (III), which is hydrolyzed with NaOH in refluxing ethanol to the corresponding free acid (IV). The reaction of (IV) with methylmagnesium iodide in ether yields 2-(2-isopropyl-5-indanyl)-2-hydroxypropionic acid (V), which is dehydrated with H2SO4 in refluxing dioxane affording 2-(2-isopropyl-5-indanyl)acrylic acid (VI) (1,2,4). Finally this compound is reduced with H2 over Raney-Ni or Pd/C in methanol or dioxane

参考文献No.900217
标题:
作者:Payne, T.G. (Hexachimie SA)
来源:CH 605564
合成路线图解说明:

The Friedel-Kraft抯 reaction of 2-isopropylindan (I) with ethyloxalyl chloride (II) by means of AlCl3 in methylene chloride gives ethyl 2-(2-isopropyl-5-indanyl)-2-oxoacetate (III), which is hydrolyzed with NaOH in refluxing ethanol to the corresponding free acid (IV). The reaction of (IV) with methylmagnesium iodide in ether yields 2-(2-isopropyl-5-indanyl)-2-hydroxypropionic acid (V), which is dehydrated with H2SO4 in refluxing dioxane affording 2-(2-isopropyl-5-indanyl)acrylic acid (VI) (1,2,4). Finally this compound is reduced with H2 over Raney-Ni or Pd/C in methanol or dioxane

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