Process for the Preparation of Eserethole

PCT No. PCT/EP93/01353 Sec. 371 Date Dec. 19, 1994 Sec. 102(e) Date Dec. 19, 1994 PCT Filed May 28, 1993 PCT Pub. No. WO93/24455 PCT Pub. Date Dec. 9, 1993.Eserethole of formula (VII) is prepared from 1,3-dimethyl-5-hydroxy-oxindole compound II which is acylated in the first step to obtain 1,3-dimet...

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Hauptverfasser:	MAIORANA, STEFANO, CHIODINI, GIORGIO, BELLI, ALDO
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS APPARATUS THEREFOR CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOIDCHEMISTRY CHEMISTRY GENERAL METHODS OF ORGANIC CHEMISTRY HETEROCYCLIC COMPOUNDS METALLURGY ORGANIC CHEMISTRY PERFORMING OPERATIONS PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL THEIR RELEVANT APPARATUS TRANSPORTING
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Zusammenfassung:	PCT No. PCT/EP93/01353 Sec. 371 Date Dec. 19, 1994 Sec. 102(e) Date Dec. 19, 1994 PCT Filed May 28, 1993 PCT Pub. No. WO93/24455 PCT Pub. Date Dec. 9, 1993.Eserethole of formula (VII) is prepared from 1,3-dimethyl-5-hydroxy-oxindole compound II which is acylated in the first step to obtain 1,3-dimethyl-5-acyloxyoxindole (III). The product is reacted with chloroacetonitrile to obtain 1,3-dimethyl-3-cyanomethyl-5-acyloxy-oxindole (IV). The 5-acyloxy group is hydrolyzed and the hydroxy group is ethoxylated with ethyl halides or sulfate. Then the product is cyclized by treatment with sodium bis-(methoxy-ethoxy)aluminum hydride, to give O-ethyl-nor-eseroline (VI) and the compound is methylated to give eserethole (VII).