Process|Asymmetric synthesis solution of alogliptin preparation process

Alogliptin Benzoate (Alogliptin Benzoate) is a serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor under Takeda, Japan.

Figure 1 Alogliptin (1) initial synthesis process

The initial synthesis process of Alogliptin is shown in Figure 1.

Figure 2 Alogliptin (1) improved process

The improved Alogliptin is shown in Figure 2.

Next, Intermediate 8 and Compound 9 undergo substitution reaction under basic conditions to obtain Intermediate 10; Intermediate 10 undergoes Hofmann rearrangement reaction under the catalysis of iodobenzene diacetic acid (PIDA) to obtain Compound 1, which is carried out by process developers.

Figure Three Trigliptin succinate Trelagliptin (12) Succinate synthesis

It is worth mentioning that the researchers used a similar process to achieve the efficient synthesis of another DPP4 inhibitor-Trelagliptin Succinate (Figure 3).

DPP4 is a key enzyme that promotes the degradation and inactivation of GLP-1 in vivo and in vitro.

The new process has found asymmetric synthesis solution for alogliptin, which provides a strong guarantee for the market demand of alogliptin.

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