Published 1964 | Version v1
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Synthesis of phenobarbital 14C - 5 (1964)

Creators

  • 1. Commissariat a l'Energie Atomique, Saclay (France). Centre d'Etudes Nucleaires

Description

Phenobarbital (Luminal), well known as a hypnotic agent, plays also an important role in the medical treatment of epilepsy. With the object of studying the metabolism of this medicament in the living system, the synthesis of phenobarbital marked in position 2 of the pyrimidinic ring has been effected. It has been necessary, in order to carry out to research into the metabolism of this product, to have a phenobarbital marked in position 5 of the pyrimidinic ring. This synthesis, making it possible to introduce C-14 into position 5 of the pyrimidinic ring, consists of seven stages starting from C-14 carboxyl benzoic acid having a specific activity of 25 mc/mM. The melting point of the final product is 172 - 173 deg. C and its specific activity is 11.15 mc/mM. The overall radioactive yield of the pure product, with respect to the original benzoic acid (10 mM) is of the order of 3 per cent. The purity of the product has been controlled by paper chromatography; it is of the order of 99 per cent. (author)

Availability note (English)

Available from INIS in electronic form

Abstract (French)

Le phenobarbital (Luminal) bien connu comme agent hypnotique, joue egalement un role important dans la medication anti-epileptique. Pour l'etude du metabolisme de ce medicament dans l'organisme vivant, nous avons synthetise le phenobarbital marque en position 2 du cycle pyrimidinique. Afin de poursuivre la recherche du metabolisme de ce produit, il a ete necessaire de disposer du phenobarbital marque en position 5 du cycle. pyrimidinique. Cette synthese, permettant l'introduction du 14C en position 5 du cycle pyrimidinique, comporte sept etapes, au depart de l'acide benzoique carboxyle 14C, d'une activite specifique de 25 mc/mM. Point de fusion du produit final: 172 - 173 deg. C Activite specifique: 11,15 mC/mM. Rendement total radioactif du produit pur, par rapport a l'acide benzoique de depart sur 10 mM, de l'ordre de 3 pour cent. La purete du produit a ete controlee par chromatographie sur papier; elle est de l'ordre de 99 pour cent. (auteur)

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Additional details

Additional titles

Original title (French)
Synthese du phenobarbital

Publishing Information

Imprint Pagination
19 p.
Report number
CEA-R--2406

INIS

Country of Publication
France
Country of Input or Organization
France
INIS RN
37064750
Subject category
S38: RADIATION CHEMISTRY, RADIOCHEMISTRY AND NUCLEAR CHEMISTRY;
Descriptors DEI
BENZOIC ACID; CARBON 14 COMPOUNDS; CHEMICAL PREPARATION; GAS CHROMATOGRAPHY; LABELLED COMPOUNDS; METABOLISM; PHENOBARBITAL
Descriptors DEC
ANESTHETICS; ANTICONVULSANTS; AZINES; BARBITURATES; CARBON COMPOUNDS; CARBOXYLIC ACIDS; CENTRAL NERVOUS SYSTEM AGENTS; CENTRAL NERVOUS SYSTEM DEPRESSANTS; CHROMATOGRAPHY; DRUGS; HETEROCYCLIC COMPOUNDS; HYPNOTICS AND SEDATIVES; LABELLED COMPOUNDS; MONOCARBOXYLIC ACIDS; ORGANIC ACIDS; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANIC OXYGEN COMPOUNDS; PYRIMIDINES; SEPARATION PROCESSES; SYNTHESIS

Optional Information

Notes
3 refs.