Method for the preparation of hexahydroazepinones and hexahydroa

Details Method for the preparation of hexahydroazepinones and hexahydroa Method for the preparation of hexahydroazepinones and hexahydroa

1994-12-19

1998-06-02

Shah, Mukund J.

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

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

540553, 540604, C07D26702, C07D28102, C07D24300, C07D22308

Patent

active

057602212

ABSTRACT:
This disclosure describes two technical procedures for the high-yield synthesis of heterocyclic seven-membered ring-systems by Dieckmann-condensation avoiding usual dilution techniques and long reaction times. Thus, it significantly increases the overall yields of the pharmaceutically active ingredients azelastine and flezelastine, whose synthesis, starting from these seven-membered heterocyclic rings, is reported elsewhere. Yields range from 80-89%, avoiding waste and increasing economics of the synthesis.

REFERENCES:
patent: 3813384 (1974-05-01), Vogelsang et al.
Scheffler et al., "Synthese und Kristallstrukturanalyse von Azelastin", Arch. Pharm. (Weinheim), vol. 321, 1988, pp. 205-208.
John Wiley & Sons, Inc., Organic Reactions, vol. 15, 1967, pp. 1-13, p. 40.
Published by the Chemical Society of Japan, vol. 31, No. 4, May 1958, pp. 418-422.
Collection of Czechoslovak Chemical Communications, vol. 51, 1986, pp. 2034-2049.

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