439910-96-0

Usage

Pyrimidine derivative

A compound that is derived from the pyrimidine ring structure This indicates that the compound is based on the pyrimidine structure, which is a six-membered heterocyclic ring system.

Amino group

A functional group with the formula -NH2 This indicates the presence of an amino group, which is a common functional group in organic chemistry that can participate in various reactions.

Building block in organic synthesis

Used as a starting material in the synthesis of more complex organic compounds This suggests that the compound is often used as a starting material in organic synthesis, which can lead to the creation of more complex molecules.

Pharmaceutical research

Has potential applications in the development of new drugs and pharmaceuticals This suggests that the compound may have potential applications in the pharmaceutical industry, possibly due to its structural features or biological activities.

Hazardous properties

Should be handled with care and follow proper safety protocols This indicates that the compound may have hazardous properties and should be handled with caution to ensure safety.

Upstream product

• 32683-07-1 N-carboxymethylbenzamidine 
• 204461-07-4 5-acetylamino-6-oxo-2-phenyl-1(6H)-pyrimidineacetic acid 
• 777047-83-3 C₁₃H₁₈N₂O₂ 
• 331985-92-3 N-(tert-butoxycarbonylmethyl)benzamidine hydrochloride 
• 634148-47-3 5-(benzoylamino)-6-oxo-2-phenyl-1(6H)-pyrimidineacetic acid tert-butyl ester 

Relevant academic research and scientific papers

Syntheses of 5-amino-2-phenyl-4(3H)-pyrimidinone derivertives starting with glycine

N-Cbz derivative of 5-amino-2-phenyl-4(3H)-pyrimidinone was prepared from sodium salt of methyl hydroxymethylene glycinate and benzamidine hydrochloride in good yield. However, the reaction with N-substituted benzamidine did not proceed to give the desired pyrimidinone. In contrast, the reaction of 4-ethoxymethylene-2-phenyl-5(4H)-oxazolone readily prepared from hippuric acid and N-substituted benzamidine proceeded nicely to give 5-(benzoylamino)-6-oxo-2- phenyl-1(6H)-pyrimidineacetic acid in high yield.

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.

PROCESS FOR PRODUCING PYRIMIDINE COMPOUND

Azlactone Compound (2) is reacted with Amidine Compound (3) to give Pyrimidine Compound (1) useful as an intermediate for enzyme inhibitors (e.g., elastase inhibitor, chymase inhibitor etc.): Pyrimidine Compound (1) Azlactone Compound (2) Amidine Compound (3) wherein each symbol is as defined in the specification.

PYRIMIDINE DERIVATIVES AND PROCESS FOR PREPARING THE SAME

A pyrimidine derivative compound of formula (I) or a salt thereof and a method for the preparation thereof.The pyrimidine derivative of formula (I) or a salt thereof is useful as important synthetic intermediate for a pharmaceutical a drug. The method for