Process for the preparation of pyrrolidone derivatives

Details Process for the preparation of pyrrolidone derivatives Process for the preparation of pyrrolidone derivatives

1988-03-08

1989-01-10

Brust, Joseph Paul

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548301, 560 39, 560169, C07D20712

Patent

active

047974966

ABSTRACT:
Process for preparing pyrrolidinone derivatives of (1) ##STR1## in which R is hydrogen, alkyl or acyl characterized in that a compound of (2) ##STR2## wherein R.sup.1 is hydrogen and R.sup.2 is benzyl or substituted benzyl, or R.sup.1 and R.sup.2 can together form a group ##STR3## where R.sup.4 and R.sup.5 are independently hydrogen, alkyl, phenyl or optionally substituted aryl or together are 1,4-butylene or 1,5-pentylene; R.sup.3 is hydrogen or straight or branched alkyl of 1 to 4 carbon atoms; and X is alkyl subjected to N-deprotection and the deprotected intermediate is cyclized intramolecularly.
The deprotected intermediates can be isolated as acid-addition salts.

REFERENCES:
patent: 4118396 (1978-10-01), Pifferi et al.
patent: 4124594 (1978-11-01), Monguzzi et al.
patent: 4173569 (1979-11-01), Banfi et al.
patent: 4476308 (1984-10-01), Aschwanden et al.
Noller, Chemistry of Organic Compounds, 3rd Ed. (1965), pp. 813-814.
Pifferi et al., Il Farmaco (Ed. Sc.) 32: 602-613 (1977).

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