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Synthese de la [(p-Chlorophenyl)-2′ Phenylacetyl-14C-1′]-2 Indanedione-1, 3 - Chlorophacinone Marquee au 14C

✍ Scribed by L. Pichat; J. Tostain; E. Boschetti

Publisher
John Wiley and Sons
Year
1978
Tongue
French
Weight
287 KB
Volume
15
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

The carbonation with lPCO2 of the lithium derivative 6 prepared from p-chtorcdiphenytmethane 5 and n-but 1 lithium in THF i n presence of tetramethylmediamine gives (~4C-carbozyt) 2-I -chi!oro phenyll-2-phenylacetic acid 7 with 85 X yield based on d04.

Action of thionyl chloride gave the corresponding chloride which l ~a s condensed with the lithium reagent derived from trimethytsityt malonate 9 leading after hydrolysis t o l-(p-chlorophenyl)-l henyl 2-prdpanone-2-14C 4 with an overall yield of 72 X baeed on 3C02.

The ketone 4 reacted with met 1 hthatate gave r i s e t o 2-((2'-p-~i n o n e -~~c ) .

OVemZt yietd based on 14Co2 was 36 Xspecific a c i t i v i t y : 15 mCi/mMole. chtorophenyl) phenytacetyt-I I-78 CI-I, d-indane dione 1 (chloropha-La ((p-chlorophenyl)-2' phenylacetyl)-2 indane dione-1.3 1 e s t un puissant raticide, agissant par abaissement du taux de prothrombine du sang. qui a ete brevet6 des 1960 (1) e t est comnercialise sous l e nom de chlorophacinone (2).

La societe LIPHA nous a demand6 de r e a l i s e r l a synthese de l a chlorophaci-A. Meynaud e t E. Boschetti (3) ont deja prepare ce r a t i c i d e marque au 14C none marquee au carbone 14.

sur l e groupe carbonyl du groupe phenylacetyl. Le schema reactionnel I , nonpublie, u t i l i s e par ces auteurs. e s t pour l'essentiel, identique a c e l u i de l a preparation i n d u s t r i e l l e de l a chlorophacinone (1). 0362-4803/78/00 15-O023%0 1-00 01978 by John Wiley & Sons Ltd.

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