Waste sitagliptin syntheses

A comparison of the amount of waste produced per kilogram of sitagliptin manufactured by the two processes demonstrates the improved efficiency of the new route (Figure 5.6). Overall, the new route reduces the total waste output of the process by approximately 80%. This will result in over 220000 kg less waste per 1000 kg of sitagliptin produced. While the first-generation synthesis produced over 60 L of aqueous waste per kg of 1, the new route produces no aqueous waste only 2 liters of water per kg of sitagliptin is now required for its preparation. 

Second-generation synthesis creates 2201b less waste for each pound of sitagliptin manufactured. 

Merck has discovered a more efficient catalytic synthesis for sitagliptin, a chiral (3-amino acid derivative that is the active ingredient in their new treatment for type 2 diabetes, Januvia . This revolutionary synthesis creates 220 pounds less waste for each pound of sitagliptin manufactured, and increases the overall yield by nearly 50%. Over the lifetime of Januvia , Merck expects to eliminate the formation of at least 330 million pounds of waste, including nearly 110 million pounds of aqueous waste. 

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