US 2025/0353810 A1 · PROCESS FOR THE PREPARATION OF TROFINETIDE

Abstract

Present invention relates to Trofinetide of Formula I having a purity of 99.0% or more and one or more of each of compound of Formula II, compound of Formula A, compound of Formula B, compound of Formula C, compound of Formula D, compound of Formula E, or compound of Formula F, which when present, is in a detectable amount of about 0.15% or less, as measured by area percentage of HPLC. In particular, the present invention relates to novel intermediate compound of Formula II, process for the preparation of novel intermediate and use of novel intermediate compound in the preparation of trofinetide. Present invention further relates to use of trofinetide in the preparation of composition comprising trofinetide.

Claims16

Dependent claims

1-11. (canceled)

A process for the preparation of trofinetide, or salts, or hydrates thereof, the process comprising:

(a) reacting a compound of Formula VII,
with N-Hydroxysuccinimide in the presence of one or more reagents to obtain a compound of Formula VI;
(b) reacting the compound of Formula VI with a compound of Formula V or salts thereof,
in the presence of one or more bases to obtain a compound of Formula IV;
(c) reacting the compound of Formula IV with a compound of Formula III or salts thereof,
in the presence of one or more reagents to obtain a compound of Formula II;
(d) deprotecting the compound of Formula II with a reagent to obtain trofinetide and
(e) optionally, converting trofinetide obtained in step (d) to salts or hydrates thereof.

5 more elements

Dependencies are inferred from the claim text.

Process for the preparation of trofinetide

Life of this patent

Process for the preparation of trofinetide

Life of this patent

Abstract

Claims16