The synthesis of Tirzepatide mainly adopts the strategy of solid-phase fragment condensation and solid-liquid binding, which focuses on solving the static hindrance effect of unnatural amino acids (such as Aib) in its 39 amino acid long chains, complex modifications of side chains (such as C20 diacid-PEG-γ-Glu-double AEEA-Lys²⁰), and racemic impurity control. The following are specific synthesis methods and technical points:

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