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Development of a Novel and Scalable Process for the Synthesis of a Key Cangrelor Intermediate

Cangrelor (Figure 1) is a parenteral drug that reversibly inhibits the P2Y12 receptor; like ticagrelor, it does not require metabolic activation. It has a rather short half-life of 3 to 4minutes; and, with an infusion of 4mg/kg per minute, peak inhibition occurs after 15minutes. Cangrelor also has a rapid offset, with normal levels of platelet aggregation returning after 60minutes. Inhibitors of platelet activation and aggregation are substances that are useful during percutaneous coronary intervention and other catheterization techniques in order to reduce bleeding complications and in the treatment of acute coronary syndromes and clotting disorders in general. One class of antiplatelet agents includes the inhibitors of the P2Y12 receptor, a G-protein coupled purinergic receptor which is an important component of platelet activation. Cangrelor (trade name kengreal in the US and kengrexal in Europe) was approved by the United States Food and Drug Administration in 2015. In continuation of our ongoing research to improve the process and identify impurities we now report a novel, convenient, and readily scalable approach for the synthesis of the key intermediate of cangrelor. A detailed study has been undertaken to identify, synthesize and characterize the cangrelor intermediates using up-to-date spectral techniques (IR, NMR, and HRMS). The synthesis of cangrelor has been reported in the literature starting from 2mercaptoadenosine (Scheme 1). The synthesis involves seven stages and additional purifications to get cangrelor. During the synthesis, compound 5 serves as a key precursor. This material is highly expensive. The reported preparation of this compound involves four steps. However, the preparation suffers from certain drawbacks, most importantly the availability of the starting material as being difficult to access. A lot of purification procedures were involved in each stage, and these present difficulties in scale-up. Therefore, a synthetic route starting from more readily available and cheaper substrates was sought. The synthetic process reported in the literature shows that the