Phil A Skone

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Aryl aminopyrazole amides capped with N-alkylbenzamides 13-16 are selective glucocorticoid receptor agonists. 2,6-Disubstituted benzamides have prednisolone-like potency or better in vitro. Good oral exposure was demonstrated in the rat, with compounds with lower lipophilicity, for example N-hydroxyethyl benzamides (e.g., 16e).
When 2'-O-methoxytetrahydropyranyl-5'-O-(9-phenylxanthen-9-yl) uridylyl-(3'----5')-(2',3'-di-O-acetyluridine) 2-chlorophenyl ester (9) is treated with zinc bromide in dichloromethane-propan-2-ol (85:15 v/v) at room temperature, under stringently anhydrous conditions, the corresponding 5'-unblocked dinucleoside phosphate (10) is obtained in 86% isolated(More)
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