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2005
Thiophene derivatives
R 0090
Solution-Phase Parallel Synthesis of a 1140-Member Ureidothiophene Carboxylic
Library. — With a view to pharmaceutical use, the title library is synthesized by
31- 118 Acid
reaction of a set of 60 primary or secondary amines like (II) with an aqueous suspension
of 18 thieno[3,2-d]oxazines of type (I) or thieno[2,3-d]oxazine (IV). Acidification of
the reaction mixture leads to precipitation of the target acids as solids, each product in
a 200—400-mg scale with over 70% yield. — (LE FOULON, F.-X.; BRAUD, E.;
FABIS, F.; LANCELOT, J.-C.; RAULT*, S.; J. Comb. Chem. 7 (2005) 2, 253-257;
Cent. Etud. Rech. Med. Normandie, UFR Sci. Pharm., Univ. Caen, F-14032 Caen, Fr.;
Eng.) — Klein
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