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Thienopyrimidine compound or pharmaceutically acceptable salt thereof as well as preparation method and application of thienopyrimidine compound or pharmaceutically acceptable salt thereof

A compound and pyrimidine technology, applied in the field of thienopyrimidine compounds or their pharmaceutically acceptable salts and their preparation, can solve the problems of less research on KRASG12D and the like, and achieve the effect of good effect and good anti-tumor activity

Active Publication Date: 2022-05-27
GUANGDONG CHENKANG BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In recent years, studies on KRAS mutations have mainly focused on KRAS G12C, and few studies on KRAS G12D

Method used

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  • Thienopyrimidine compound or pharmaceutically acceptable salt thereof as well as preparation method and application of thienopyrimidine compound or pharmaceutically acceptable salt thereof
  • Thienopyrimidine compound or pharmaceutically acceptable salt thereof as well as preparation method and application of thienopyrimidine compound or pharmaceutically acceptable salt thereof
  • Thienopyrimidine compound or pharmaceutically acceptable salt thereof as well as preparation method and application of thienopyrimidine compound or pharmaceutically acceptable salt thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1 provides a thienopyrimidine compound, and the structural formula of the thienopyrimidine compound is shown in formula (I):

[0038]

[0039] Its preparation method comprises the following steps:

[0040] Compound 1 (247.88 mg), compound 2 (212.15 mg) and N,N-diisopropylethylamine (90 mg) were added to N,N-dimethylformamide (2 mL) for reaction to obtain compound 3, the compound 3. Suzuki reaction is carried out to obtain compound 4, and compound 4 is removed BOC under hydrochloric acid conditions, and the solvent is spin-dried to obtain compound (I);

[0041] Wherein the preparation of compound 4:

[0042] Compound 3 (424.06 mg) and 2-methoxy-5-trifluoromethylbenzeneboronic acid (219.95 mg) were added to N,N-dimethylformamide, and 7 mg of tetrakistriphenylphosphine palladium and 300 mg of sodium carbonate were added. The reaction was carried out under the conditions of , and compound 4 was obtained by column chromatography;

[0043] The structural form...

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PUM

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Abstract

The invention discloses a thienopyrimidine compound or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The structural formula of the thienopyrimidine compound is shown as a formula (I), and the thienopyrimidine compound disclosed by the invention can be combined with KRAS G12D and has an inhibiting effect on tumor proliferation of KRAS G12D mutation.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a thienopyrimidine compound or a pharmaceutically acceptable salt thereof and a preparation method and application thereof. Background technique [0002] The murine sarcoma virus oncogene (RAS) protein is an important member of the GTPases family, including NRAS, HRAS and KRAS. These enzymes play important roles in extracellular signal transduction, proliferation, apoptosis and differentiation. KRAS binds to guanine trinucleotide phosphate (GTP) in an active conformation and binds to guanine dinucleotide phosphate (GDP) in an inactive conformation. The tight binding of mutated KRAS protein and GTP puts the KRAS protein in an abnormal persistent activation conformation, resulting in persistent activation of downstream signaling pathways. KRAS inhibitors produce antitumor activity by recognizing mutant KRAS, blocking KRAS / GEF interaction, and inhibiting KRAS...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00A61K31/519A61P35/00
CPCC07D519/00A61P35/00Y02P20/55
Inventor 不公告发明人
Owner GUANGDONG CHENKANG BIOTECHNOLOGY CO LTD