PROCESS FOR PREPARING PERHYDRO IMIDAZO THIAZOLE DERIVATIVES

PROCESS FOR PREPARING PERHYDRO IMIDAZO THIAZOLE DERIVATIVES

Title derivs. I (R, X = Et, O; Pr, O; Et, S; Pr, S) were prepd. by amidating-cyclization of II (R1 = H, alkyl). Fungicidal data of I were given against Botrytis cinerea and Cochliobolus miyabeanus. Thus, a mixt. of HSCH2CH2NH2;HCl 11.4, Et3N 10.1, and 2-oxobutyric acid 10.2 g in EtOH was refluxed 30...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: SHIGEMATSU TAICHIRO, YOSHIDA KENJI, KASUGAI HIROSHI, NAKAZAWA MAKOTO
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Title derivs. I (R, X = Et, O; Pr, O; Et, S; Pr, S) were prepd. by amidating-cyclization of II (R1 = H, alkyl). Fungicidal data of I were given against Botrytis cinerea and Cochliobolus miyabeanus. Thus, a mixt. of HSCH2CH2NH2;HCl 11.4, Et3N 10.1, and 2-oxobutyric acid 10.2 g in EtOH was refluxed 30 min to give 65.7% 2-ethylthiazolidine-2-carboxylic acid (III), which was refluxed with 20% HCl/MeOH 30min to give 18.4% III Me ester (IV). Stirring 0.62 g IV with 0.66g 3,5-Cl2C6H3NCO in PhMe 1 hr at room temp. gave 77.8% II (R = Et, R1 = Me, X = O), which was heated in 0.1 N NaOMe/MeOH 20 min at 50 C give 25% I (R = Et; X = O).