62190-98-1Relevant 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
Takahashi, Daisuke,Izawa, Kunisuke,Kashiwagi, Tatsumi,Onoye, Hiromi,Williams, Robert M.
, p. 2213 - 2229,17 (2020/08/31)
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.
PROCESSES FOR PRODUCTION OF PYRIMIDINE DERIVATIVES AND INTERMEDIATES
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Page/Page column 32, (2010/11/23)
Compound (I) is reacted with compound (II) to give compound (III), which is then reacted with compound (IX) to give compound (VIII), which is then preferably deprotected by an enzyme reaction to give compound (XII). The present invention provides an advan
Azlactone compound and method for preparation thereof
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Page/Page column 9, (2008/06/13)
The present invention provides a preparation method of a compound represented by the formula (II): wherein M is a hydrogen atom, sodium, potassium or lithium, P is a hydrogen atom, an alkyl group and the like and a wavy line shows a cis form, a trans form
Production method of pyrimidine derivative, intermediate therefor
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Page/Page column 38, (2010/02/11)
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
Production method of aminopyrimidine compound
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Page/Page column 10, (2008/06/13)
Aminopyrimidine compounds represented by formula (3) may be efficiently prepared by reacting an azlactone compound represented by formula (1) with an amidine compound represented by formula (2) or a salt thereof: wherein R1, R2 and M are as defined in the specification.
