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US 12,006,324 B1Granted
Preparation method of trilaciclib and precursors of trilaciclib
AssigneeChunghwa Chemical Synthesis & Biotech Co. Ltd.
InventorsSatyanarayana Kamani, Hsin-Yun Chang, Tzu-Chiang Lu, Chin-Cheng Mai
Life of this patent
Estimating the term…
Abstract
Disclosed herein is a specific method of preparation of Trilaciclib. The said method is to provide an efficacy of a protection free synthetic method of Trilaciclib with less steps and good yields.
Claims21
A method for preparing Trilaciclib of formula (I),
- comprising:
- (a) oxidizing a compound of formula (VII) to afford a compound of formula (VI-1) or (VI-2);
- (b) reacting a compound of formula (V) and the compound of formula (VI-1) or (VI-2) under a strong alkali to afford a compound of formula (IV);
- (c) conducting an intramolecular cyclization of the compound of formula (IV) in presence of a base to afford a compound of formula (III);
- (d) activating a hydroxyl group of the compound of formula III to become a leaving group to afford a compound of Formula II;
- (e) conducting a reductive elimination of the compound of formula II to afford Trilaciclib of formula (I);
- wherein
- R1 is selected from hydrogen or C1˜C4 alkyl, aryl;
- R2 is selected from hydrogen, silyl, halo alkyl, —C(O) alkyl, —S(O)2 alkyl, —S(O)2 halo alkyl, —S(O)2 aryl or —S(O)2 aryl-alkyl.
6 more elements
A compound of formula (II),
- wherein R2 is selected from hydrogen, silyl, halo alkyl, —C(O) alkyl, —S(O)2 alkyl, —S(O)2 halo alkyl, —S(O)2 aryl or —S(O)2 aryl-alkyl.
A compound of formula (III),
A compound of formula (IV),
- wherein R1 is selected from hydrogen or C1˜C4 alkyl.
Dependencies are inferred from the claim text.