1220518-04-6

Basic information

• Product Name: 2,4-dichloro-7-cyclopropyl-7H-pyrrolo[2,3-d]pyriMidine
• Synonyms: 2,4-dichloro-7-cyclopropyl-7H-pyrrolo[2,3-d]pyriMidine
• CAS NO: 1220518-04-6
• Molecular Formula: C₉H₇Cl₂N₃
• Molecular Weight: 228.08
• Mol File: 1220518-04-6.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 2,4-dichloro-7-cyclopropyl-7H-pyrrolo[2,3-d]pyriMidine(CAS DataBase Reference)
• NIST Chemistry Reference: 2,4-dichloro-7-cyclopropyl-7H-pyrrolo[2,3-d]pyriMidine(1220518-04-6)
• EPA Substance Registry System: 2,4-dichloro-7-cyclopropyl-7H-pyrrolo[2,3-d]pyriMidine(1220518-04-6)

Safety Data

• Hazardous Substances Data: 1220518-04-6(Hazardous Substances Data)

Usage

General Description

2,4-dichloro-7-cyclopropyl-7H-pyrrolo[2,3-d]pyrimidine is a chemical compound that belongs to the pyrrolopyrimidine class of molecules. It is a heterocyclic aromatic compound consisting of a pyrrole ring fused to a pyrimidine ring, with two chlorine atoms and a cyclopropyl group attached to the pyrimidine ring. 2,4-dichloro-7-cyclopropyl-7H-pyrrolo[2,3-d]pyrimidine has potential applications in the pharmaceutical industry, particularly in the development of new drugs. It may exhibit biological activity as a kinase inhibitor or have other therapeutic properties. Its structure and unique properties make it an interesting target for research and potential drug development.

Upstream product

• 4333-56-6 cyclopropyl bromide 
• 90213-66-4 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine 
• 411235-57-9 cyclopropylboronic acid 

Relevant articles and documents

Design, synthesis and biological evaluation of sphingosine-1-phosphate receptor 2 antagonists as potent 5-FU-resistance reversal agents for the treatment of colorectal cancer

5-Fluorouracil (5-FU) and its prodrugs are the essential clinical drugs for colorectal cancer (CRC) treatment. However, the drug resistance of 5-FU has caused high mortality of CRC patients. Thus, it is urgent to develop reversal agents of 5-FU resistance. Sphingosine-1-phosphate receptor 2 (S1PR2) was proved to be a potential target for reversing 5-FU resistance, but the activity of known S1PR2 antagonists JTE-013 were weak in 5-FU-resistant cell lines. To develop more potent S1PR2 antagonists to treat 5-FU-resistant cancer, a series of JTE-013 derivatives were designed and synthesized. The most promising compound 40 could markedly reverse the resistance in 5-FU-resistant HCT116 cells and 5-FU-resistant SW620 cells via inhibiting the expression of dihydropyrimidine dehydrogenase (DPD). The key was that compound 40 with improved pharmacokinetic properties significantly increased the inhibitory rate of 5-FU in the SW620/5-FU cells xenograft model with no observable toxicity by inhibiting the expression of DPD in tumor and liver tissues. Altogether, these results suggest that compound 40 may be a promising drug candidate to reverse 5-FU resistance in the treatment of CRC.

Discovery of 1-methyl-1 H-imidazole derivatives as potent Jak2 inhibitors

Structure based design, synthesis, and biological evaluation of a novel series of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT pathway, are described. Using the C-ring fragment from our first clinical candidate AZD1480 (24), optimization of the series led to the discovery of compound 19a, a potent, orally bioavailable Jak2 inhibitor. Compound 19a displayed a high level of cellular activity in hematopoietic cell lines harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound 19a demonstrated significant tumor growth inhibition in a UKE-1 xenograft model within a well-tolerated dose range.

HETEROCYCLIC JAK KINASE INHIBITORS

The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer