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1
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13044276784
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note
-
(a) The majority of the analogues, whose preparation and in vitro evaluation are described in this study, are novel tricyclic GPIIb/IIIa antagonists. However, the preparation and in vitro evaluation of one novel tetracyclic GPIIb/IIIa antagonist is also included,
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2
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13044266903
-
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Anaheim, CA.; Abstract 229, MEDI
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(b) A portion of the work described herein, as well as SAR of additional tricyclic IIbIIIa antagonists containing a nonoptimized arginine surrogate, was presented at the 209th National ACS Convention, Anaheim, CA.; Abstract 229, MEDI.
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209th National ACS Convention
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A Receptor, U.S. Patent 5,663,166 1997. For preparation of 18, see page 219 of U.S. Patent 5,663,166. In the base mediated ring closure to yield 19, cesium carbonate (1.2 equiv., DMF, rt) was also a suitable base. The procedure to prepare 19 using sodium hydride to promote 7-member ring formation is described on page 220 of U.S. Patent 5,663,166
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(a) TCI supplies > 98% purity N-methyl isatoic anhydride which provides products in much greater purity and yield than the use of technical grade N-methyl isatoic anhydride.
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(b) 1.0 M KPhos buffer (pH 7) was prepared by mixing 1.0 M potassium phosphate monobasic and 1.0 M potassium phosphate dibasic until pH 7.0 (approximately 1:1.2 ratio).
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