US4128547-6 - (D-α-氨基 - 对 - hydroxyphenylacetamido) - 青霉烷酸制备.pdf

United States Patent [19] [11] 4,128,547 van der Drift et al. [45] Dec. 5, 1978 [54] I6-(D-a-AMINO-P-HYDROXY- ‘ [57] ABSTRACT PHENYLACETAMIDO)-PENICILLANIC A process for the preparation of 6-(D-a-amino-p ACID PREPARATION hydroxyphenylacetamido)-penicillanic acid or amox [75] Inventors: Johannes K. van der Drift, Delft; icillin by reacting 6-aminopenicillanic acid with at least Peter W. Henniger, Leiden; Gerard J. two equivalents of a silylating agent producing trimeth van Veen, Pijnacker, all of ylsilyl groups in an anhydrous, inert, water-insoluble Netherlands organic solvent and reacting the resulting product at a temperature below —25° C with an at least equimolar [73] Assignee: Gist-Brocades N.V., Delft, amount of a compound of the formula Netherlands [21] Appl. No.: 854,821 [22] Filed: Nov. 25, 1977 x [30] Foreign Application Priority Data 001. 31, 1977 [JP] Japan 52-130694 Sep. 6, 1977 [NL] Netherlands 7709812 [51] Int. Cl.2 C07D 499/12; C07D 499/04 [52] US. Cl. 260/2391 wherein R1 and R7 are lower alkoxy, R2 is lower alkyl [58] Field of Search 260/239.1 and R3 is selected from the group consisting of lower [56] References Cited alkyl and hydrogen previously prepared f