61369-26-4

Upstream product

• 500-98-1 phenylacetylglycine 
• 122-51-0 orthoformic acid triethyl ester 
• 64-67-5 diethyl sulfate 
• 332095-91-7 2-benzyl-4-hydroxymethylene-5-oxazolinone 
• 52616-42-9 (+/-)-2-(C-phenyl-acetylamino)-3.3-diethoxy-propionic acid 

Downstream Products

• 25439-22-9 N-(2-morpholin-4-yl-2-oxo-ethyl)-2-phenyl-acetamide 
• 855416-52-3 2-benzyl-4-morpholinomethylen-4H-oxazol-5-one 

Relevant academic research and scientific papers

An improved synthesis of 5-acylamino-6-oxo-2-phenyl-1(6h)-pyrimidineacetic acid from glycine with readily removable protecting groups

Concise synthesis of N-acyl-5-amino-6-oxo-2-phenyl-1(6H)- yrimidineacetic acid was achieved by cyclization reaction of 2-alkyl-4- lkoxymethylene-5(4H)- oxazolone with N-(carboxymethyl)benzamidine, while a similar reaction with sodium salt of 2-alkyl-4-hydroxymethylene-5(4H)- xazolones gave a mixture of regioisomers of the pyrimidinone. N-Acyl groups (acetyl or phenylacetyl) of the pyrimidinone derivatives were readily cleaved under very mild conditions with weak base or enzyme. Thus, the process enabled us to synthesize the drug candidate without exchanging N-protecting group. Since the starting oxazolones were easily prepared from N-acylglycine, the synthetic route can be used for the large scale synthesis of the key intermediate for several enzyme inhibitors.

Production method of pyrimidine derivative, intermediate therefor

The present invention relates to a production method of compound (XV), which includes hydrolysis of compound (I) to give compound (II), then reaction with reagent (III) to give compound (IV), then reaction with compound (V) to give compound (VI), then con