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Primary Examiner: Demers, Arthur P.
Assistant Examiner:
Attorney: Sprung, Felfe, Horn, Lynch & Kramer

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Title: Dioxopiperazine derivatives suitable for use as medicaments and .beta.-lactam antibiotic intermediates

Abstract: New dioxo-piperazine derivatives suitable for use as medicaments and .beta.-lactam antibiotic intermediates of the formula ##STR1## in which Z is ##STR2## and, R.sup.1 and R.sup.2 each independently is hydrogen or various optionally substituted aliphatic, aromatic or heterocyclic radicals or together form an optionally substituted ring, are formed by reacting (a) 1-amino-2,3-dioxo-piperazine of the formula ##STR3## with a compound of the formula ##STR4## or a hydrate, acetal, ketal, sulphite, hydrogen halide or hydrocyanic acid addition product thereof or, ##STR5## with an oxalic acid ester in the presence of a diluent, thereby to effect cyclization. The new derivatives are anti-virally active and can also be chlorocarbonated with phosgene to form a reactive derivative which can be condensed with the amino group of .alpha.-amino penicillins to form antibiotics.

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Inventors: Preiss, Michael (Wuppertal, DE, US)

Application Number: 861473
Filing Date: 1977-12-16
Publication_date: 1980-01-08
Assignee: Bayer Aktiengesellschaft (Leverkusen, DE)
Primary Class(es): 514/252.13 514/254.04, 514/254.1, 514/255.02, 544/382, 544/385
Other Classes:
US Patent Ref:

3183229	May, 1965	Cusic et al.	544/382.
3746704	Jul, 1973	Kollmeyer et al.	542/420.
3803136	Apr, 1974	Schwan et al.	542/420.
3830805	Aug, 1974	Pilgram	542/420.
3903081	Sep, 1975	Winkelmann	544/382.
3978068	Aug, 1976	Dickore et al.	542/425.
4049650	Sep, 1977	White	542/420.

Other Refs: Other References: Saikawa et al., Chem Abst. 87, (1977), #102380 #53376 and #53377.
Knobloch et al., Chem. Abstracts 58, col. 2504(b).