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A short synthesis and its application to the preparation of radio labelled leukotriene inhibitor Sch 37224

✍ Scribed by T. Duelfer; D. Gala

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
263 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

A -new, short synthesis of 1 -(1.2-dihydro-4-hydroxy-l -phenyl-2-0x0-I ,8naphthyridin-3-yl)-pyrrolidinium hydroxide, inner salt. 1, was achieved by condensing methyl 2-phenylamino-3-pyridine carboxylate 2 with ethyl 1 -pyrrolidine acetate 4. This gave highly pure product in 60% yield. This synthesis was applied to the preparation of 14C labelled 1. Radiolabelled 1 was synthesized from u-[14C]-aniline in three steps at 97% radiochemical purity and 27.3% radiochemical yield.

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