4-(2-phenoxyethyl)-1,2,4-triazolone process intermediates

Details 4-(2-phenoxyethyl)-1,2,4-triazolone process intermediates 4-(2-phenoxyethyl)-1,2,4-triazolone process intermediates

1985-06-03

1986-06-24

Helfin, Bernard

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

548263, C07C125067

Patent

active

045968845

ABSTRACT:
An improved process for the preparation of 5-ethyl-4-(2-phenoxyethyl)-1,2,4-triazolone, a useful intermediate in the synthesis of antidepressant 1,2,4-triazolones typified by 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxethyl)-2 H-1,2,4-triazol-3(4H)-one, also known as nefazodone. The improved process is shorter and higher in yield than the former process, and the starting materials are cheap and readily available.

REFERENCES:
patent: 4318731 (1982-03-01), Kajioka et al.
patent: 4487773 (1984-12-01), Temple et al.
Dow Technical Bulletin, "Developmental 2-Ethyl-2-Oxazoline XAS-1454, Ethyloxazoline: An Intermediate for Aminoethylation".
W. Reid and Z. Czack, Ann., 676, pp. 121-129 (1964).
M. Pesson, et al., Bull Soc. Chim., Fr., pp. 1367-1371 (1962).

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