Pyridine Loratadine

Loratadine (ll-[N-carboethoxy-4-piperidylidene]-8-chloro-6,ll-dihydro-5H-benzo-[5,6]-cyclohepta-[l,2-b]-pyridine) is an antihistamine. U.S. 4,282,233 (to Sobering) describes the preparation of the API and also gives recipes for syrup (Example 6) and tablet (Example 7) formulations. Estimate the cost of the making the API and both formulations. 

Loratadine. 4 i8-Chloro-Sf6-dihydro-l lH bettzo [bjcyctoh epta[I, 2 bJpyridi n -11 -y f i den e) t-p f peri di n cca rb-oxylic acid ethyl ester ll-l/V- ethoxycarbonyl)-4-piperidyl-idene]-8-chlorO-6,l l -dihydrO-Sif-benzo cyclohepta-tl 2-6]pyridine Sch-29851 Clantin CLaritin Clarityne Lisino. C HjjClNjOji mol wt 3 2.89. C 69 01%, H 6,05%, Cl 9 26%, N 7-32%, O 8.36%. Nonsedating-type histamine H.-receptor antagonist. Prepn F. J. Vtllani, U.S. pat. 

The privileged pyridine scaffold is present in a large number of marketed drugs including esomeprazole (Nexium), loratadine (Claritin), and the recently approved cancer therapeutic crizotinib (Xalkori). Sabitha and coworkers have developed the first general method for the synthesis of... 

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