【药物名称】Encainide, MJ-9067-1(hydrochloride), MJ-9067, Enkaid
化学结构式(Chemical Structure):
参考文献No.46010
标题:Process for production of encainide
作者:Madding, G.D. (Bristol-Myers Squibb Co.)
来源:JP 58105963; NL 8204775; US 4394507
合成路线图解说明:

A new method for the synthesis of encainide has been reported: The acylation of methyl anthranilate (I) with 4-anisoyl chloride (II) by means of NaOH in methylene chloride gives methyl N-(p-anisoyl)anthranilate (III), which is condensed with 2-picoline (IV) by means of n-butyllithium in THF yielding 2-(2-pyridylacetyl)-p-anisanilide (V). Finally, this compound is reduced with H2 over Pt/C then with Pd/C, treated with formaldehyde and reduced again with H2 over Pt/C.

参考文献No.49264
标题:MJ 9067
作者:Casta馿r, J.
来源:Drugs Fut 1977,2(3),176
合成路线图解说明:

The condensation of 2-methylpyridine (I) with 2-nitrobenzaldehyde (II) in acetic anhydride gives 2-(2-nitrostyryl)pyridine (III), which is quaternized with methyl iodide in refluxing acetone yielding 2-(2-nitrostyryl)-1-methylpyridinium iodide (IV) . The reduction of (IV) with H2 over PtO2 in ethanol affords 2-(2-aminophenethyl)-1-methylpiperidine (V), which is then acylated with 4-methoxybenzoyl chloride (A) in pyridine.

参考文献No.607784
标题:Lysergic acid and quimidine analogs. 2-(o-Acylaminophenethyl)piperidines
作者:Dykstra, S.J.; Minielli, J.L.; Lawson, J.E.; Ferguson, H.C.; Dungan, K.W.
来源:J Med Chem 1973,16(9),1015
合成路线图解说明:

The condensation of 2-methylpyridine (I) with 2-nitrobenzaldehyde (II) in acetic anhydride gives 2-(2-nitrostyryl)pyridine (III), which is quaternized with methyl iodide in refluxing acetone yielding 2-(2-nitrostyryl)-1-methylpyridinium iodide (IV) . The reduction of (IV) with H2 over PtO2 in ethanol affords 2-(2-aminophenethyl)-1-methylpiperidine (V), which is then acylated with 4-methoxybenzoyl chloride (A) in pyridine.

参考文献No.800693
标题:Substituted piperidines and a process for the preparation thereof
作者:Dykstra, S.J.; Minielli, J.L.
来源:BE 0779951; CA 961038; CH 578529; DE 2210154; FR 2128584; GB 1346261; NL 161443C; NL 7202614
合成路线图解说明:

The condensation of 2-methylpyridine (I) with 2-nitrobenzaldehyde (II) in acetic anhydride gives 2-(2-nitrostyryl)pyridine (III), which is quaternized with methyl iodide in refluxing acetone yielding 2-(2-nitrostyryl)-1-methylpyridinium iodide (IV) . The reduction of (IV) with H2 over PtO2 in ethanol affords 2-(2-aminophenethyl)-1-methylpiperidine (V), which is then acylated with 4-methoxybenzoyl chloride (A) in pyridine.

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