1374639-75-4

Basic information

• Product Name: LEE011 (succinate)
• Synonyms: LEE011 (succinate);7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate;LEE-011 succinate salt, Ribociclib succinate salt;Ribociclib succinate
• CAS NO: 1374639-75-4
• Molecular Formula: C27H36N8O5
• Molecular Weight: 552.62534
• Mol File: 1374639-75-4.mol
• Article Data: 16

Chemical Properties

• Appearance: /
• Storage Temp.: Refrigerator
• Solubility: DMSO (Slightly), Methanol (Slightly)
• CAS DataBase Reference: LEE011 (succinate)(CAS DataBase Reference)
• NIST Chemistry Reference: LEE011 (succinate)(1374639-75-4)
• EPA Substance Registry System: LEE011 (succinate)(1374639-75-4)

Safety Data

• Hazardous Substances Data: 1374639-75-4(Hazardous Substances Data)

Usage

Uses

LEE011 is an orally bioavailable and highly specific CDK4/6 (cyclin-dependent kinase 4/6) inhibitor. LEE011 in combination with LGX818 (a V600E BRAF specific inhibitor) or BYL719 (a PIK3CA specific inhibitor) leads to robust anti-tumor activity in melanoma and breast cancer tumor models.

Upstream product

• 1003-03-8 Cyclopentamine 
• 110-15-6 succinic acid 
• 1211441-98-3 (7-cyclopentyl-Ν,Ν-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo [2,3-d]pyrimidine-6-carboxamide) 
• 571188-59-5 tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate 
• 571189-16-7 4-(6-nitropyridin-3-yl)-piperazine-1-carboxylic acid tert-butyl ester 
• 733039-20-8 5-bromo-2-chloro-N-cyclopentylaminopyrimidine-4-amine 
• 1211443-61-6 2-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide 
• 1374639-76-5 3-(2-chloro-4-(cyclopentylamino)pyrimidin-5-yl)prop-2-yn-1-ol 
• 1374639-78-7 N,N‐dimethyl‐7‐cyclopentyl‐2‐{[5‐(4-tert-butoxycarbonylpiperazin‐1‐yl)pyridin‐2‐yl]amino}‐7H‐pyrrolo[2,3‐d]pyrimidine‐6‐carboxamide 
• 39856-50-3 5-bromo2-nitropyridine 
• 1374639-77-6 (2-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl)methanol 
• 52092-47-4 5-chloro-2-nitropyridine 
• 775288-71-6 1-(6-nitropyridin-3-yl)piperazine 
• 1195-08-0 2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carbaldehyde 

Relevant articles and documents

PREPARATION METHOD OF RIBOCICLIB AND ITS SALT AND CRYSTALLINE FORM THEREOF

The present invention provides a preparation method of ribociclib and its salt and a novel crystalline form of ribociclib succinate. The conditions of the preparation method of the present invention are easier than the conventional process, and the yield is higher as well. The purity of ribociclib in crude product stage meets the requirement for quality of active pharmaceutical ingredient (API), so that no further purification is required. The crystalline form of ribociclib succinate in the present invention has outstanding storage stability.

RIBOCICLIB INTERMEDIATE AND PROCESS FOR PREPARATION THEREOF

The present invention relates to the process for the preparation of ribociclib succinate by making use of novel intermediates. The invention also relates to the process for the preparation of novel intermediates.

NOVEL POLYMORPHS OF RIBOCICLIB SUCCINATE

The present invention relates to novel crystalline forms of Ribociclib Succinate and its preparation process.