107347-90-0Relevant articles and documents
Production process of 5-(3, 3-dimethylguanidino)-2-oxopentanoic acid
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, (2020/07/02)
The invention discloses a production process of 5-(3,3-dimethylguanidino)-2-oxopentanoic acid. The 5-(3,3-dimethylguanidino)-2-oxopentanoic acid is prepared by connecting two fragments; the first fragment is prepared by the following steps: carrying out a substitution reaction on diethyl oxalate, serving as an initial raw material, and 1,4-butyrolactone to generate an intermediate 1, carrying outa ring-opening bromination reaction on the intermediate 1 and an acetic acid solution of hydrobromic acid to obtain an intermediate 2, and carrying out an esterification reaction on the intermediate 2and methanol to prepare an intermediate 3; and the second fragment is prepared by reacting N,N'-bis-BOC-1H-1-guanidinopyrazole serving as an initial raw material with a methanol solution of dimethylamine to obtain an intermediate 4. An alkylation substitution reaction on the intermediates 4 and 3 to prepare an intermediate 5, the intermediate 5 is deprotected to obtain an intermediate 6, and ester is hydrolyzed to obtain the target product. By establishing strict internal control standards for initial raw materials and intermediates and strictly controlling key process step parameters, the qualified product can be stably prepared in multiple batches.
