PREPARATION OF 5-(2-(DIMETHYLAMINO)ETHOXY)CARVACROL

Title:

PREPARATION OF 5-(2-(DIMETHYLAMINO)ETHOXY)CARVACROL

Document Type and Number:

Japanese Patent JPS58126844

Kind Code:

A

Abstract:

PURPOSE: To prepare the titled compound which is a synthetic intermediate of thymoxamine hydrochloride useful as a medicine of cardio-vasocular organ, easily, in a short step, in high yield and purity, using a compound derived from thymol in two steps, via a Grignard compound.

CONSTITUTION: 2-Bromo-5-[ 2-(dimethylamino)ethoxy ]-p-cymene of formulaIis made to react with Mg, and the resultant Grignard compound of formula II is made to react with trialkyl borate of formula B(OR)3 (R is lower alkyl) to obtain a boron derivative of formula III (m and n are positive integer; m+n=3). The objective compound of formula IV can be obtained by oxidizing the boron derivative with H2O2.

EFFECT: There is little generation of N-oxide in the oxidation with H2O2 irrespective of the presence of tert-amino group at the side chain.

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Inventors:

KUTSUMA TERUO
SEKINE YASUO
KAKUIRI AKIHITO

Application Number:

JP752882A

Publication Date:

July 28, 1983

Filing Date:

January 22, 1982

Export Citation:

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Assignee:

FUJI ZOKI SEIYAKU

International Classes:

C07C217/34; C07C67/00; C07C213/00; (IPC1-7): C07C93/06

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