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Synthesis of aldose reductase inhibitor, 3,4‐dihydro‐4‐oxo‐3‐[[5‐(trifluoromethyl)‐2 14 C benzothiazolyl]methyl]‐1‐phthalazineacetic acid
Author(s) -
Mylari Banavara L.,
Zembrowski William J.
Publication year - 1991
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580290204
Subject(s) - chemistry , trifluoromethyl , hydrolysis , aldose reductase inhibitor , aldose , stereochemistry , acid hydrolysis , organic chemistry , aldose reductase , medicinal chemistry , enzyme , glycoside , alkyl
Synthesis of the title compound, C 14 labeled CP‐73,850 (zopolrestat), was accomplished by condensation of 1‐phthalazineacetic acid, 3,‐ 14 C cyanomethyl‐3,4‐dihydro‐4‐oxo‐, ethyl ester with 3‐amino‐4‐mercapto‐benzotrifluoride, followed by base hydrolysis of the resultant product, 1‐phthalazineacetic acid, 3,4‐dihydro‐4‐oxo‐3‐[[5‐trifluoromethyl)‐2‐benzothiazolyl] 14 C methyl]‐3,4‐dihydro‐4‐oxo‐, ethyl ester.