5305-40-8

Usage

Uses

Used in Pharmaceutical Industry:
4,6-Dichloro-5-pyrimidinecarbaldehyde is used as a substrate for the synthesis of N-terminal surrogates in amino acid and peptide analogues. These analogues are essential in the development of new drugs and therapeutic agents, particularly for various medical conditions. 4,6-Dichloro-5-pyrimidinecarbaldehyde's unique structure allows for the creation of novel molecules with potential applications in treating diseases and improving patient outcomes.

InChI:InChI=1/C13H12N2O/c1-10-5-4-8-13(15-10)14-9-11-6-2-3-7-12(11)16/h2-9H,1H3,(H,14,15)/b11-9-

Upstream product

• 1193-24-4 4,6-pyrimidinediol 
• 1193-21-1 4,6-dichloropyrimidine 
• 68-12-2 N,N-dimethyl-formamide 
• 14256-99-6 4,6-dihydroxy-5-formylpyrimidine 
• 1193-24-4 6-hydroxy-3,4-dihydropyrimidin-4-one 

Downstream Products

• 54503-94-5 4-chloro-6-morpholin-4-yl-pyrimidine-5-carbaldehyde 
• 251989-01-2 4,6-bis[4-(tert-butyl)phenoxy]pyrimidine-5-carbaldehyde 
• 251989-02-3 4,6-bis[3,5-di(tert-butyl)phenoxy]pyrimidine-5-carbaldehyde 
• 60025-05-0 4,6-dichloro-5-(α-hydroxyethyl)pyrimidine 
• 64127-14-6 2-[1-(2-hydroxy-ethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino]-benzoic acid 
• 947661-83-8 methyl 4-((6-chloro-5-formylpyrimidin-4-yl)(4-methoxybenzyl)amino)butanoate 
• 14160-96-4 4-chloro-6-(phenylamino)pyrimidine-5-carbaldehyde 
• 650637-99-3 4-chloro-1-(pyridin-2-yl)-1H-pyrazolo[3,4-d]pyrimidine 
• 885524-07-2 4-chloro-1-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidine 
• 1100365-43-2 C₁₁H₇ClN₄ 
• 5334-48-5 4-chloro-1-(phenyl)-1H-pyrazolo[3,4-d]pyrimidine 
• 35877-38-4 4-chloro-1-benzyl-1H-pyrazolo[3,4-d]pyrimidine 
• 650628-54-9 4-chloro-1-(4-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidine 
• 1100365-46-5 C₁₁H₅Cl₃F₃N₅ 

Relevant academic research and scientific papers

Design, synthesis and evaluation of pyrrolo[2,3-d]pyrimidine-phenylamide hybrids as potent Janus kinase 2 inhibitors

Janus kinase 2 (JAK2) plays an essential role in the signaling of hormone-like cytokines and growth factors, which has been convinced as an important target of myeloproliferative neoplasms (MPNs) therapy. In this study, a series of novel pyrrolo[2,3-d]pyr

Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors

A series of novel 4,5,6-trisubstituted pyrimidines were designed as potent covalent Bruton's tyrosine kinase (BTK) inhibitors based on the structure of ibrutinib by using a ring-opening strategy. Among these derivatives, compound I1 exhibited the most potent inhibitory activity with an IC50 value of 0.07 μM. The preliminary structure-activity relationship was discussed and the primary amino group at the C-4 position of pyrimidine was crucial for maintaining BTK activity. Furthermore, molecular dynamics simulations and binding free energy calculations were performed for three inhibitor-BTK complexes to determine the probable binding model, which provided a comprehensive guide for further structural modification and optimization.

PROCESS AND INTERMEDIATES FOR PREPARING A JAK1 INHIBITOR

The present invention is related to processes for preparing itacitinib, or a salt thereof, and related synthetic intermediates related thereto.

PROCESS AND INTERMEDIATES FOR PREPARING A JAK INHIBITOR

The present invention is related to processes for preparing ruxolitinib, or a salt thereof, and related synthetic intermediates related thereto.

1H-PYRAZOLO[3,4-D]PYRIMIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF PLATINUM-RESISTANT CANCER

The invention relates to compounds of formula (I) and related compounds and their use in the treatment of cancer, especially platinum resistant cancer. The invention also provides a treatment comprising administration of a compound of formula (I) and a pl

PROCESSES AND INTERMEDIATES FOR MAKING A JAK INHIBITOR

This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.

HETEROARYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSTION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers, autoimmune diseases, and respiratory diseases.

Preparation methods of JAK inhibitor and salt thereof

The present invention relates to preparation methods of a JAK inhibitor and a salt thereof. The preparation method comprises: (1) carrying out a Suzuki coupling reaction on (R)-3-(4-boronic acid-1H-pyrazol-1-yl)-3-cyclopentylpropionitrile and 6-halogen-5-(2-methoxyvinyl)pyrimidin-4-ylamine to generate (3R)-cyclopentyl-3-[4-(5-(2-methoxyvinyl)pyrimidin-4-ylamine)pyrazol-1-yl]propionitrile; and (2)carrying out a protection group removing and ring-closure reaction on the (3R)-cyclopentyl-3-[4-(5-(2-methoxyvinyl)pyrimidin-4-ylamine)pyrazol-1-yl]propionitrile to generate a JAK inhibitor ruxolitinib. According to the present invention, the new ruxolitinib preparation route is provided, wherein each reaction of the route has the high yield, the total yield of the route is high, the purity of theobtained product is good, the post-treatment of the reaction is simple, and column chromatography is not required; by adopting the route, the required raw materials or catalysts and other materials are relatively easy to obtain; and compared to the method in the prior art, the method of the present invention is economical and is suitable for industrial production.

Intermediate of JAK inhibitor, and preparation method thereof

The present invention relates to a novel key intermediate of a JAK inhibitor ruxolitinib, and a preparation method thereof, wherein the chemical name of the intermediate is (R)-3-(4-boric acid-1H-pyrazole-1-yl)-3-cyclopentylpropionitrile. According to the present invention, the new ruxolitinib preparation route is provided, wherein each reaction of the route has the high yield, the total yield ofthe route is high, the purity of the obtained product is good, the post-treatment of the reaction is simple, and column chromatography is not required; by adopting the route, the required raw materials or catalysts and other materials are relatively easy to obtain; and compared to the method in the prior art, the method of the present invention is economical and is suitable for industrial production.

4-Aminopyrimidine compound, and preparation method and medicinal use thereof

The invention belongs to the field of medicines, and concretely relates to a 4-aminopyrimidine compound having a structural represented by formula (I), or pharmaceutically acceptable salts thereof, a preparation method of the compound, and a use of the compound and the salts as a Bruton tyrosine kinase (BTK) inhibitor. A result of experiments shows that the compound has a significant inhibition effect on the BTK, and can be used for treating thromboembolism, inflammatory disorders, autoimmune diseases, Waldenstrom macroglobulinemia, B cell lymphomas and other diseases.