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We report a facile synthesis of the angiotensin II type 2 receptor antagonist EMA401, which recently passed phase II clinical trials, in high overall yield. The synthesis of the key phenylalanine intermediate involved the formation of an α-nitro cinnamic ester and its reduction followed by a Pictet–Spengler cyclization, which furnished the tetrahydroisoquinoline core structure. Next, EMA401 was separated...
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