REPARATION OF ARYL (OR HETEROARYL) PIPERAZINYLBUTYLAZOLE DERIVATIVE

Japanese Patent JP3084537

B2

PURPOSE: To provide the method for the preparation of aryl (or heteroaryl) piperazinylthiazole derivative with high yield, which has pharmacological activities against central nervous systems.
CONSTITUTION: The compound of formula III, e.g. 1-{4-[4-(2-pyrimidinyl)-1- piperazinyl]butyl}pyrrole is obtained by allowing a compound of formula I [Ar is a (substituted) aryl, (substituted) 2-pyrimidine, 2-N-methylimidazole, 3-(1,2- benzoisothiazole); X is a halogen] to react with a compound of formula II [Z1 is N or C-R1; Z2 is N or C-R2; Z3 is N or C-R4; R1 to R4 may form a part of another aromatic ring or non-aromatic ring, or are each H, a halogen, alkyl, NO2, OH, alkoxy, CN, carboxyl, carboxamide, alkylcarboxylate, (substituted) aryl, sulfonyl, sulfonamide or (substituted) amino] in an appropriate solvent preferably in the presence of a base (preferably potassium carbonate) at 80-160°C.

Ramon Merce Vidal
Georges Frigola Constanta
Fan Palace Colominas

JP4996492A

September 04, 2000

March 06, 1992

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Laboratorios del Doctor Esteve, S.A.

A61K31/435; A61K31/495; A61K31/496; A61K31/505; A61P9/12; A61P25/00; A61P25/20; A61P25/24; A61P25/26; A61P25/28; C07D207/32; C07D207/325; C07D231/12; A61K31/40; C07D231/16; C07D231/20; C07D231/38; C07D231/56; C07D233/61; C07D233/68; C07D239/26; C07D241/04; C07D277/64; C07D403/12; C07D403/14; C07D417/12; C07D471/04; C07D521/00; (IPC1-7): C07D207/32; C07D231/38; C07D233/61; C07D233/68; C07D403/12; C07D417/12; C07D471/04

JP4234387A

Kakehi Yuro (2 outside)

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