34171-40-9

Usage

Uses

Used in Pharmaceutical Industry:
2,4-dichloro-5-ethylpyrimidine is used as a reactant for the synthesis of pyrimidine derivatives, which have various applications in the pharmaceutical industry. These derivatives act as inhibitors of dipeptidyl peptidase IV (DPP-IV), a proteolytic enzyme that plays a role in glucose regulation. Inhibiting DPP-IV can help manage blood sugar levels and is beneficial for the treatment of type 2 diabetes.
Additionally, 2,4-dichloro-5-ethylpyrimidine is used in the synthesis of pyrimidine derivatives that target TBK1/IKKε kinases. These kinases are involved in the regulation of immune responses and are potential therapeutic targets for the treatment of autoimmune diseases and inflammation.
Furthermore, 2,4-dichloro-5-ethylpyrimidine is utilized in the development of inhibitors for the hedgehog signaling pathway, which is crucial for embryonic development and tissue regeneration. Abnormal activation of the hedgehog pathway has been associated with various cancers, making it a potential target for cancer therapy.

Upstream product

• 4212-49-1 5-ethyluracil 
• 34171-37-4 5-ethyl-2-thiouracil 
• 63857-18-1 2-formyl-butyric acid methyl ester 

Downstream Products

• 111196-81-7 2-chloro-5-ethylpyrimidine 
• 1349584-37-7 cyclobutanecarboxylic acid {3-[5-ethyl-2-(3-fluoro-phenylamino)-pyrimidin-4-ylamino]-propyl}-amide 
• 1352570-81-0 2-chloro-5-ethyl-4-(4-methoxybenzyloxy)pyrimidine 
• 1352571-52-8 5-ethyl-2-(2-isopropoxy-6-(4-(methylsulfonyl)phenoxy)pyridin-4-yl)-4-(4-methoxybenzyloxy)pyrimidine 

Relevant academic research and scientific papers

Discovery of a potent and highly isoform-selective inhibitor of the neglected ribosomal protein s6 kinase beta 2 (S6k2)

The ribosomal protein S6 kinase beta 2 (S6K2) is thought to play an important role in malignant cell proliferation, but is understudied compared to its closely related homolog S6 kinase beta 1 (S6K1). To better understand the biological function of S6K2, chemical probes are needed, but the high similarity between S6K2 and S6K1 makes it challenging to selectively address S6K2 with small molecules. We were able to design the first potent and highly isoform-specific S6K2 inhibitor from a known S6K1-selective inhibitor, which was merged with a covalent inhibitor engaging a cysteine located in the hinge region in the fibroblast growth factor receptor kinase (FGFR) 4 via a nucleophilic aromatic substitution (SNAr) reaction. The title compound shows a high selectivity over kinases with an equivalently positioned cysteine, as well as in a larger kinase panel. A good stability towards glutathione and Nα-acetyl lysine indicates a non-promiscuous reactivity pattern. Thus, the title compound represents an important step towards a high-quality chemical probe to study S6K2-specific signaling.

Indole pyrimidine compound as well as synthesis method and application thereof

The invention discloses an indole pyrimidine compound, the structural formula of which is as shown in formula (I): wherein L is selected from any one of H, OH, halogen, alkoxy, halogenated alkyl, alkyl, aryl and pyridine, Q is O, S or NH, X is NH or -CONH, n is a natural number, R is N(CH3)2 or T is selected from at least one of H, OH, halogen, alkoxy, halogenated alkyl, alkyl, aryl and pyridine. The indole pyrimidine compound provided by the invention can effectively inhibit adipocyte differentiation, and has a better lipid-lowering effect.

Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases

The design, synthesis and structure-activity relationships of a novel series of 2,4-diamino-5-cyclopropyl pyrimidines is described. Starting from BX795, originally reported to be a potent inhibitor of PDK1, we have developed compounds with improved selectivity and drug-like properties. These compounds have been evaluated in a range of cellular and in vivo assays, enabling us to probe the putative role of the TBK1/IKKε pathway in inflammatory diseases.

Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV

The discovery of two classes of heterocyclic dipeptidyl peptidase IV (DPP-4) inhibitors, pyrimidinones and pyrimidinediones, is described. After a single oral dose, these potent, selective, and noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes. Compounds 13a, 27b, and 27j were selected for development.

Preparation of C-5 substituted cidofovir derivatives

1-[(S)-3-Hydroxy-2-(phosphonomethoxy)propyl]cytosine (HPMPC, cidofovir) was modified by substitution on the base moiety in positions C-S and N4. Key intermediates of these syntheses, diisopropyl esters of (S)-1-[2-(phosphonomethoxy)-3-(tripheny

QUINOLINE, TETRAHYDROQUINOLINE AND PYRIMIDINE DERIVATIVES AS MCH ANTAGONIST

The present invention relates to compounds of the Formula (I) wherein Q is: which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

PYRIMIDO COMPOUNDS HAVING ANTIPROLIFERATIVE ACTIVITY (II)

Disclosed are novel pyrimido compounds of the formula (I) wherein R1 to R9 are as defined in the specification, that are selective inhibitors of the Src family of tyrosine kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, hepatic and pancreatic tumors. Also disclosed are pharmaceutical compositions containing these compounds and the use for treating cancer.

Synthesis of 5-ethyl-2-pyrimidinone-2'-deoxyriboside as a new potential antiviral agent

5-Ethyl-2-pyrimidinone (5) and its 2'-deoxyribosides 9 (α) and 10 (β) have been synthesized in several steps starting from 5-ethyluracil. 10 is presented for evaluation against herpes virus infection.

The facile synthesis of N(1),N(4)-dimethyl-5-substituted cytosines

A facile, high yield synthesis of N(1),N(4)-dimethyl-5-alkyl (methyl, ethyl, n-propyl, n-butyl) cytosines has been described. This method seems to be an alternative and universal route to N(1),N(4)-methylated cytosines with any 5-substituent.