The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Apr. 07, 1981
Filed:
Dec. 31, 1979
Ajay K Bose, Mountain Lakes, NJ (US);
Gist-Brocades N.V., Delft, NL;
Abstract
Novel process for the preparation of .beta.-lactams of the formulae: ##STR1## wherein R' represents lower alkyl, aryl or aryl (lower alkyl), R' represents hydrogen or lower alkyl or R' and R' together with the carbon atoms to which they are attached represent lower cycloalkyl, R'' represents lower alkyl or a group --OR, wherein R represents lower alkyl, X.sub.1, Y.sub.1 and Z.sub.1 are hydrogen or selected organic radicals and R.sub.1 represents an acyl group; which successively involves reacting an 1,3-dicarbonyl compound of the formula: ##STR2## with glycine in the presence of a base to form a vinylamino salt of the formula: ##STR3## wherein M.sub.1.sup.+ is the cation of the base, activating the carboxyl group of said vinylamino salt with an appropriate activating agent and reacting the activated compound in the presence of a tertiary base with an imino compound of the formula: ##STR4## to form the corresponding .alpha.-vinylamino-.beta.-lactam of formula IV A and if desired, subjecting said .beta.-lactam to mild acid hydrolysis to obtain the corresponding .alpha.-amino-.beta.-lactam of formula V A and if desired, acylating said .alpha.-amino-.beta.-lactam with an appropriate acylating agent to obtain a corresponding .alpha.-acylamino-.beta.-lactam of formula VI A.