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First-pass effect: Nonlinear concept comprising an explicit solution of integrated Michaelis-Menten equation

✍ Scribed by Frieder Keller; Jürgen Scholle


Publisher
John Wiley and Sons
Year
1981
Tongue
English
Weight
397 KB
Volume
70
Category
Article
ISSN
0022-3549

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✦ Synopsis


solution of VII as the free base (1.96 g, 0.013 mole) in 50 ml of tetrahydrofuran was treated with triethylamine (1.27 g, 0.013 mole), followed by the dropwise addition of methanesulfonyl chloride (1.43 g, 0.013 mole).

The reaction mixture was stirred at room temperature for 4 hr and fdtered to remove the precipitated triethylamine hydrochloride. The filtrate was evaporated under reduced pressure to yield a light-yellow oil. Column chromatography of the oil using silica gel as the adsorbent and chloroform-methanol (91) as the solvent gave, after evaporation of the solvents, 0.77 g (26%) of a white crystalline solid. An analytical sample was obtained by recrystallization from chloroform-hexane to give white crystals, mp 82-83O; IR (KBr): 3300 (NH), 1785 (C=O, imide), 1710 (C=O, imide), and 1150 (SO2) cm-'; NMR 6 0.90 (t, 3H,