C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/264.3
C07D 237/32 (2006.01)
Patent
CA 1300142
0231/DLR5 17599IA TITLE OF THE INVENTION Improved Process for the Preparation of 3-[(4-Bromo-2- fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazine- acetic Acid. ABSTRACT OF THE DISCLOSURE There is disclosed an improved process for the preparation of 3-[(4-bromo-2-fluorophenyl)- methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid. The process is significantly improved over the prior art process in preparing the product in a one-step process where the prior art required three steps. The instant process directly alkylates a phthalazine ring nitrogen in the presence of the acetic acid moiety without the necessity of protecting the carboxylic acid group as was necessary in the prior art preferred process. The product is useful for treating the progressive deterioration resulting from diabetes, and is of the general formula: Image
586458
Gowling Lafleur Henderson Llp
Merck & Co. Inc.
Shuman Richard F.
LandOfFree
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