362656-23-3

Usage

Uses

Used in Pharmaceutical Industry:
8-cyclopentyl-5-Methyl-2-(Methylthio)pyrido[2,3-d]pyriMidin-7(8H)-one is used as a potential drug candidate for its ability to interact with biological targets, which may contribute to the development of new therapeutic agents.
Used in Anti-cancer Therapies:
In the field of oncology, 8-cyclopentyl-5-Methyl-2-(Methylthio)pyrido[2,3-d]pyriMidin-7(8H)-one is used as a potential anti-cancer agent, with its structure possibly allowing it to modulate various oncological signaling pathways and exhibit inhibitory effects on tumor growth and progression.
Used in Anti-inflammatory Therapies:
8-cyclopentyl-5-Methyl-2-(Methylthio)pyrido[2,3-d]pyriMidin-7(8H)-one is also considered for use in anti-inflammatory therapies, where its molecular structure may contribute to the mitigation of inflammation by interacting with specific biological targets.
Further research and study of 8-cyclopentyl-5-Methyl-2-(Methylthio)pyrido[2,3-d]pyriMidin-7(8H)-one are necessary to fully understand its potential applications and to develop effective drug delivery systems that can enhance its bioavailability and therapeutic outcomes.

Upstream product

• 362656-11-9 1-(4-cyclopentylamino-2-methylsulfanylpyrimidin-5-yl)ethanone 
• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 
• 5909-24-0 4-chloro-2-methanesulfanylpyrimidine-5-carboxylic acid ethyl ester 
• 1003-03-8 Cyclopentamine 
• 211245-64-6 4-cyclopentylamino-2-methylsulfanyl-pyrimidine-5-carbaldehyde 
• 211245-62-4 4-cyclopentylamino-2-(methylsulfanyl)pyrimidine-5-carboxylic acid ethyl ester 
• 211245-63-5 [4-cyclopentylamino-2-(methylsulfanyl)pyrimidine-5-yl]methanol 
• 5751-20-2 2-Methylthiouracil 
• 81560-03-4 2-methylsulfanyl-5-bromopyrimidin-4-one 
• 63810-78-6 4?chloro?5?bromo?2?(methylthio)pyrimidine 
• 733039-23-1 5?bromo?N?cyclopentyl?2?(methylthio)pyrimidin?4?amine 
• 107-93-7 (E)-but-2-enoic acid 
• 49844-90-8 4-Chloro-2-methylthiopyrimidine 
• 3724-65-0 2-butenoic acid 

Downstream Products

• 362656-25-5 6-bromo-8-cyclopentyl-5-methyl-2-methylsulfanyl-8H-pyrido[2,3-d]pyrimidin-7-one 
• 571188-81-3 6?bromo?8?cyclopentyl?5?methyl?2?(methylsulfinyl)pyrido[2,3?d]pyrimidin?7(8H)?one 
• 850628-81-8 6-acetyl-8-cyclopentyl-5-methyl-2-methylsulfanyl-8H-pyrido[2,3-d]pyrimidin-7-one 
• 850628-86-3 6-acetyl-8-cyclopentyl-5-methyl-2-(methylsulfinyl)pyrido[2,3-d]pyrimidin-7(8H)-one 
• 362656-37-9 4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 850628-92-1 {1-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]pyrrolidin-3-yl}carbamic acid tert-butyl ester 
• 850628-95-4 4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]-2,2-dimethylpiperazine-1-carboxylic acid tert-butyl ester 
• 850628-93-2 4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]-[1,4]-diazepane-1-carboxylic acid tert-butyl ester 
• 850629-00-4 4-[4-(6-chloro-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 362656-71-1 4-[4-(6-bromo-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 850628-96-5 4-[2-chloro-4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 850629-03-7 4-[4-(8-cyclopentyl-6-ethyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 850628-98-7 4-[4-(8-cyclopentyl-6-iodo-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)phenyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 850629-05-9 2-[4-(4-tert-butoxycarbonylpiperazin-1-yl)phenylamino]-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid methyl ester 

Relevant academic research and scientific papers

A new route for the synthesis of Palbociclib

Abstract: In this paper, a novel synthetic method for Palbociclib was reported. It was synthesized in eight steps from 2-(methylthio) pyrimidin-4-(3H)-one with approximately 10% overall yield. This protocol started material 2-(methylthio) pyrimidin-4-(3H)-one, involved nucleophilic substitution by thionyl chloride, bromination, nucleophilic substitution by cyclopentylamine, a one pot-two step method (Heck reaction, ring close sequence), oxidation and bromination, cross-coupling reaction, Heck reaction, aqueous workup to afford Palbociclib. This synthetic route used inexpensive raw material and reagents, involved readily controllable reaction conditions and reduced environmental hazards. Graphic abstract: Synthesis of Palbociclib, a small molecule CDK inhibitor, starting from 2-(methylthio) pyrimidin-4-(3H)-one by 8 steps reaction. This method afforded the Palbociclib in 10% yield. [Figure not available: see fulltext.].

HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS

Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.

PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES AS CDK INHIBITORS

The pyrido[2,3-d]pyrimidin-7(8H)-ones of Formula (1) and pharmaceutical compositions containing compounds of Formula (1) as CDK inhibitors are disclosed herein. Methods and use of a compound of Formula 1 in the treatment of cancer and manufacture are also disclosed.

A new and efficient protocol for the synthesis of the key intermediate of palbociclib

A new and efficient synthesis of 6-bromo-8-cyclopentyl-5-methyl-2-(methylsulfinyl)-pyrido[2,3-d]pyrimidin-7(8H)-one, a key intermediate of Palbociclib, starting from thiouracil was described. This protocol involved methylation, nucleophilic substitution, bromination, nucleophilic substitution, Heck reaction, ring closure, oxidation, and bromination to afford a key intermediate of Palbociclib with approximately 35% overall yield. The advantages of this developed synthetic strategy included improved overall yield, inexpensive starting materials, and readily controllable and cleaner reaction conditions.

Method for preparing palbociclib intermediate

The invention discloses a method for preparing a palbociclib intermediate. The intermediate is 6-bromo-8-cyclopentyl-5-methyl-2-methylsulfinyl-8H-pyrido[2,3-d]pyrimidine-7-one. The method comprises the following steps: carrying out a substitution reaction on 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidine-7-one and sodium thiomethoxide to generate 8-cyclopentyl-5-methyl-2-methylsulfinyl-8H-pyrido[2,3-d]pyrimidine-7-one, and carrying out a bromination and oxidation reaction on the 8-cyclopentyl-5-methyl-2-methylsulfinyl-8H-pyrido[2,3-d]pyrimidine-7-one and N-bromosuccinimide (NBS) togenerate the palbociclib intermediate 6-bromo-8-cyclopentyl-5-methyl-2-methylsulfinyl-8H-pyrido[2,3-d]pyrimidine-7-one. The method mainly has the advantages of short synthesis route, convenience in operation, low cost of raw materials, great economic benefit and great social values.

A Palumbo vial preparation method of the key intermediate (by machine translation)

The invention discloses a Palumbo Xilin key intermediate 6 - bromo - 2 - methyl sulfonyl - 8 - cyclopentyl - 5 - methyl pyridine and (2, 3 - d) pyrimidine - 7 (8 H) - ketone. The method uses the thiourea pyrimidine as the starting material, by methylation, chloro, bromo synthesis of 5 - bromo - 4 - chloro - 2 - methylthio-pyrimidine, then with the cyclopentamine alkylation, with 2 - butenoic acid by the heck reaction, then the intramolecular acylation reaction for the synthesis of 2 - methylthio - 8 - cyclopentyl - 5 - methyl pyridine and (2, 3 - d) pyrimidine - 7 (8 H) - one, finally with the NBS reaction for the preparation of 6 - bromo - 2 - methyl sulfonyl - 8 - cyclopentyl - 5 - methyl pyridine and (2, 3 - d) pyrimidine - 7 (8 H) - one. The preparation process of the present invention short step, not using the dangerous process, simple and convenient operation, low cost of raw materials, to meet the using requirements of the people. (by machine translation)

Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6

The presently disclosed subject matter relates to methods and compositions for protecting cells and or tissues from damage due to ischemia. In particular, the presently disclosed subject matter relates to the protective action of cyclin dependent kinase 4/6 (CDK4/6) inhibitors administered to subjects that have been exposed to, or that are at risk of, ischemia.

Novel important intermediate for anticancer drug palbociclib and compounding process

The invention discloses a compounding process for a novel important intermediate for anticancer drug palbociclib. The compounding process includes allowing a compound 1 and a compound 2 to react with each other at a time with high yield under the action of Grignard reagents to obtain a compound 3, and allowing the compound 3 to react with R7CH2COOR3 to obtain a compound 4. The compounding process has a short path, and only two reaction steps, from the initial raw material 1 to the key intermediate pyridino-pyrimidine-7-ketone derivative 4, are needed; raw materials are cheap, reaction process is harmless to the environment, overall yield is high, and the compounding process is suitable for mass production.

CYCLIN DEPENDENT KINASE INHIBITORS AND METHODS OF USE

The presently disclosed subject matter relates to methods and compositions for protecting healthy cells from damage due to DNA damaging agents. In particular, the presently disclosed subject matter relates to the protective action of selective cyclin dependent kinase 4/6 (CDK4/6) inhibitors administered to subjects that have been exposed to or that are at risk of exposure to DNA damage.

Pyrimidine or pyridine pyridine ketone compound and its preparation method and application (by machine translation)

The invention discloses a kind of type I of the pyrimidine or pyridine pyridine ketone compound and its preparation and application, which belongs to the technical field of pharmaceutical preparation. The compounds have high-efficient and selectively inhibit the cell cycle dependent kinases (Cdks) CDK4 and CDK6 active, and then by inhibiting CDK4/CDK6 prevent tumor cell division. Therefore, the compounds of this invention can be used for CDK4 and CDK6 the involved in cell cycle control disorders result in various diseases, especially suitable for the treatment of malignant tumors. (by machine translation)